AMG 925

发表于2024年3月18日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AMG 925 纯度: 98.24%

AMG 925 是一种有效的选择性的 FLT3/CDK4 双重抑制剂，IC₅₀ 分别为 2±1 nM 和 3±1 nM。

AMG 925 Chemical Structure

CAS No. : 1401033-86-0

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AMG 925 相关产品

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Bioactive Compound Library Plus

生物活性

AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC₅₀s of 2±1 nM and 3±1 nM, respectively.

IC₅₀ & Target^[1]

FLT3

2 nM (IC₅₀)

CDK4

3 nM (IC₅₀)

CDK6

8 nM (IC₅₀)

CDK2

375 nM (IC₅₀)

CDK1

1.9 μM (IC₅₀)

体外研究
(In Vitro)

AMG 925 also inhibits CDK6, CDK2, and CDK1 in kinase assays with IC₅₀s of 8±2 nM, 375±150 nM, 1.90±0.51 μM, respectively. A fair overall kinase selectivity of AMG 925 is as determined by KinomScan against a panel of 442 various kinases. Cellular selectivity (on-target vs. off-target activity) of AMG 925 is about 50-fold as evaluated by comparison of its growth-inhibiting activity in RB-positive (RB⁺) and RB-negative (RB^–) non- acute myeloid leukemia (AML) cancer cell lines. AMG 925 potently inhibits growth of AML cell lines MOLM13 (FLT3-ITD; IC₅₀=19 μM) and Mv4-11 (FLT3-ITD; IC₅₀=18 μM)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

MOLM13 tumor-bearing mice are dosed twice daily by oral administration 6 hours apart with 12.5, 25, or 37.5 mg/kg AMG 925. Tumors are then harvested 3, 9, 12, and 24 hours after the first dose, and analyzed for levels of P-STAT5 and P-RB. Maximum inhibition of P-STAT5 and P-RB is achieved at 6 and 12 hours respectively at the 37.5 mg/kg dose of AMG 925. Interestingly, a rebound of P-STAT5 at 24 hours is observed, possibly as a result of compensational feedback. The pharmacodynamic responses of P-STAT5 and P-RB inhibition correlated with plasma concentrations of AMG 925. AMG 925 inhibits AML xenograft tumor growth by 96% to 99% without significant body weight loss. The antitumor activity of AMG 925 correlates with the inhibition of STAT5 and retinoblastoma protein (RB) phosphorylation, the pharmacodynamic markers for inhibition of FLT3 and CDK4, respectively. In addition, AMG 925 is also found to inhibit FLT3 mutants (e.g., D835Y) that are resistant to the current FLT3 inhibitors (e.g., AC220 and Sorafenib)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

471.55

Formula

C₂₆H₂₉N₇O₂

CAS 号

1401033-86-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

H₂O : < 0.1 mg/mL (insoluble)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

参考文献

[1]. Keegan K, et al. Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Mol Cancer Ther. 2014 Apr;13(4):880-9.

Cell Assay ^[1]	MOLM13 and Mv4-11 are used. MOLM13-Luc cells are constructed by transduction of MOLM13 cells with the pLV218G luciferin/lentivector, which expresses luciferase under the murine EF1α promoter. Sorafenib-resistant MOLM13 (MOLM13sr) and Mv4-11 (Mv4-11sr) are isolated by passaging the cells in growth medium containing increasing concentrations of Sorafenib (1-1 nM). Cell growth is measured by a DNA synthesis assay. Cells are seeded in a 96-well Cytostar T plate at a density of 5×10³ cells/well in a total volume of 160 μL. Test compounds (e.g., AMG 925; 0.03 and 0.3μM) are serially diluted into the plate (20 μL/well) and 20 μL/0.1 μCi of [¹⁴C]-Thymidine added to each well. Isotope incorporation is determined using a β plate counter after further 72-hour incubation. Apoptosis is assayed by using the Vybrant Apoptosis Assay Kit. Briefly, cells are seeded into a 6-well plate at 5×10⁵ cells per well and treated with compounds (e.g., AMG 925; 0.003, 0.01, 0.03, 0.1, 0.3, and 1 μM) for 24 hours. The cells are then stained with reagents provided in the kit and analyzed by flow cytometry. The Sytox Green fluorescence versus allophycocyanin fluorescence dot plot shows resolution of live, apoptotic, and dead cells, which are quantified using the Flowjo software. The cell-cycle analysis is done by treating the cells with AMG 925 for 24 hours followed by using the CycleTest Kit. Ten thousand events are acquired and the proportions of cells in each cycle phase are calculated using the ModFit software^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] *CrTac:NCR-Foxn1^nu* (NCR) nude mice are used. 2×10⁶ cells are innoculated on the flank of NCR nude mice and allowed to grow for 13 days. Mice are then dosed twice a day by oral administration 6 hours apart with 12.5, 25, 37.5, and 50 mg/kg of AMG 925 for 10 consecutive days^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.**
参考文献	[1]. Keegan K, et al. Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Mol Cancer Ther. 2014 Apr;13(4):880-9.

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Sovilnesib(Synonyms: AMG 650)

发表于2024年3月13日由上海金畔生物科技有限公司

Sovilnesib (Synonyms: AMG 650)

Sovilnesib (AMG 650) 是一种 kinesin-like protein KIF18A 抑制剂 (WO2020132648)。Sovilnesib 可用于癌症研究。

Sovilnesib Chemical Structure

CAS No. : 2410796-79-9

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生物活性

Sovilnesib (AMG 650) is a kinesin-like protein KIF18A inhibitor (WO2020132648). Sovilnesib can be used for the research of cancer^[1].

IC₅₀ & Target

KIF18A^[1]

体外研究
(In Vitro)

Sovilnesib is a kinesin-like protein KIF18A inhibitor^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

564.65

Formula

C₂₆H₃₄F₂N₆O₄S

CAS 号

2410796-79-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. WO2020132648

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Motesanib Diphosphate(Synonyms: AMG 706 Diphosphate)

发表于2024年3月11日由上海金畔生物科技有限公司

Motesanib Diphosphate (Synonyms: AMG 706 Diphosphate) 纯度: 99.85%

Motesanib Diphosphate (AMG 706 Diphosphate) 是一种有效的 VEGFR1/2/3 的 ATP 竞争性抑制剂，IC₅₀ 值为 2 nM/3 nM/6 nM，与对 Kit 的选择性相似，是 PDGFR 和 Ret 的 10 倍多。

Motesanib Diphosphate Chemical Structure

CAS No. : 857876-30-3

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Kinase Inhibitor Library
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Reprogramming Compound Library
Anti-Breast Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC₅₀s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.

IC₅₀ & Target^[1]

VEGFR1

2 nM (IC₅₀)

VEGFR2

3 nM (IC₅₀)

VEGFR3

6 nM (IC₅₀)

体外研究
(In Vitro)

Motesanib Diphosphate (AMG 706 Diphosphate) has broad activity against the human VEGFR family, and displays over 1000-fold selectivity against EGFR, Src, and p38 kinase.Motesanib Diphosphate (AMG 706 Diphosphate) significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC₅₀ of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC₅₀ of >3,000 nM. Motesanib Diphosphate (AMG 706 Diphosphate) also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC₅₀ of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells^[1]. Although displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib Diphosphate (AMG 706 Diphosphate) treatment significantly sensitizes the cells to fractionated radiation^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Motesanib Diphosphate (AMG 706 Diphosphate) (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED₅₀ of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib Diphosphate (AMG 706 Diphosphate) induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells^[1]. Motesanib Diphosphate (AMG 706 Diphosphate) in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models^[2]. Motesanib Diphosphate (AMG 706 Diphosphate) treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

569.44

Formula

C₂₂H₂₉N₅O₉P₂

CAS 号

857876-30-3

中文名称

二磷酸莫替沙尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : ≥ 110 mg/mL (193.17 mM)

H₂O : 5 mg/mL (8.78 mM; ultrasonic and warming and heat to 60°C)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7561 mL	8.7806 mL	17.5611 mL
5 mM	0.3512 mL	1.7561 mL	3.5122 mL
10 mM	0.1756 mL	0.8781 mL	1.7561 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 25 mg/mL (43.90 mM); Clear solution

此方案可获得 ≥ 25 mg/mL (43.90 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 250.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.39 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.39 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Polverino A, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer Res. 2006 Sep 1;66(17):8715-21.

[2]. Kruser TJ, et al. Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin Cancer Res, 2010, 16(14), 3639-3647.

[3]. Coxon A, et al. Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors. Clin Cancer Res, 2009, 15(1), 110-118.

Kinase Assay ^[1]	Optimal enzyme, ATP, and substrate (gastrin peptide) concentrations are established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib is tested in a 10-point dose-response curve for each enzyme using an ATP concentration of two-thirds K_m for each. Most assays consist of enzyme mixed with kinase reaction buffer [20 mM Tris-HCl (pH 7.5), 10 mM MgCl₂, 5 mM MnCl₂, 100 mM NaCl, 1.5 mM EGTA]. A final concentration of 1 mM DTT, 0.2 mM NaVO₄, and 20 μg/mL BSA is added before each assay. For all assays, 5.75 mg/mL streptavidin-allophycocyanin and 0.1125 nM Eu-PT66 are added immediately before the HTRF reaction. Plates are incubated for 30 minutes at room temperature and read on a Discovery instrument. IC₅₀ values are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equation. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are preincubated for 2 hours with different concentrations of Motesanib, and exposed with 50 ng/mL VEGF or 20 ng/mL bFGF for an additional 72 hours. Cells are washed twice with DPBS, and plates are frozen at -70°C for 24 hours. Proliferation is assessed by the addition of CyQuant dye, and plates are read on a Victor 1420 workstation. IC₅₀ data are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equatio. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	A431 cells are cultured in DMEM (low glucose) with 10% FBS and penicillin/streptomycin/glutamine. Cells are harvested by trypsinization, washed, and adjusted to a concentration of 5×10⁷/mL in serum-free medium. Animals are challenged s.c. with 1×10⁷ cells in 0.2 mL over the left flank. Approximately 10 days thereafter, mice are randomized based on initial tumor volume measurements and treated with either vehicle (Ora-Plus) or Motesanib. Tumor volumes and body weights are recorded twice weekly and/or on the day of sacrifice. Tumor volume is measured with a Pro-Max electronic digital caliper and calculated using the formula length (mm)×width (mm)×height (mm) and expressed in mm³. Data are expressed as mean±SE. Repeated measures ANOVA followed by Scheffe post hoc testing for multiple comparisons is used to evaluate the statistical significance of observed differences^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Polverino A, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer Res. 2006 Sep 1;66(17):8715-21. [2]. Kruser TJ, et al. Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin Cancer Res, 2010, 16(14), 3639-3647. [3]. Coxon A, et al. Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors. Clin Cancer Res, 2009, 15(1), 110-118.

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AMG-208

发表于2024年2月28日由上海金畔生物科技有限公司

AMG-208 纯度: 99.34%

AMG-208 是一种口服有效的，选择性 c-Met/RON 双抑制剂，对 c-Met 的 IC₅₀ 为 9 nM。AMG-208 是一种 CYP3A4 抑制剂，IC₅₀ 为 32 μM。AMG-208 具有抗癌活性。

AMG-208 Chemical Structure

CAS No. : 1002304-34-8

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5 mg	￥1200	In-stock
10 mg	￥1800	In-stock
50 mg	￥5400	In-stock
100 mg		询价
200 mg		询价

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AMG-208 相关产品

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Antioxidants Compound Library
Oxygen Sensing Compound Library
Anti-COVID-19 Compound Library
Orally Active Compound Library
Anti-Lung Cancer Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC₅₀ of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC₅₀ of 32 μM. AMG-208 has anti-cancer activity^[1]^[2]^[3].

IC₅₀ & Target^[1]^[2]

c-Met

9 nM (IC₅₀)

CYP3A4

32 μM (IC₅₀)

体外研究
(In Vitro)

AMG-208 (compound 4) treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC₅₀ of 46 nM^[1].
Pre-incubation of AMG-208 (compound 1) with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC₅₀ of 4.1 μM, which is an eightfold decrease relative to the IC₅₀ (32 μM) without preincubation^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

In male Sprague Dawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

383.40

Formula

C₂₂H₁₇N₅O₂

CAS 号

1002304-34-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 3.33 mg/mL (8.69 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6082 mL	13.0412 mL	26.0824 mL
5 mM	0.5216 mL	2.6082 mL	5.2165 mL
10 mM	—	—	—

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

参考文献

[1]. Albrecht BK, et al. Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase. J Med Chem. 2008, 51(10), 2879-2882.

[2]. Boezio AA, et al. Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg Med Chem Lett. 2009, 19(22), 6307-6312.

[3]. Liu X, et al. Developing c-MET pathway inhibitors for cancer therapy: progress and challenges. Trends Mol Med. 2010,16(1), 37-45.

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Murizatoclax(Synonyms: AMG 397)

发表于2024年2月11日由上海金畔生物科技有限公司

Murizatoclax (Synonyms: AMG 397)

Murizatoclax (AMG 397) 是一种有效，选择性和具有口服活性的髓样白血病 1 (MCL-1) 抑制剂，K_i 值为 15 pM。Murizatoclax 与促凋亡 BCL-2 家族成员竞争性结合 MCL1 的 BH3 结合沟。Murizatoclax 可用于癌症的研究。

Murizatoclax Chemical Structure

CAS No. : 2245848-05-7

规格	价格	是否有货
1 mg	￥92000	询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a K_i of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer^[1]^[2].

IC₅₀ & Target^[1]

MCL1

15 pM (Ki)

体外研究
(In Vitro)

AMG 397 potently disrupts the interaction between MCL1 and BIM in OPM2 cells, induces clear increases in Caspase-3/7 activity within one hour^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Murizatoclax (25-50 mg/kg; p.o. once or twice weekly) exhibits significant tumor regressions in mice bearing OPM2 xenografts^[2].
Murizatoclax (10-60 mg/kg; p.o. twice weekly) achieves 47% MOLM-13 orthotopic tumor growth inhibition (TGI), 99% TGI and 75% regression at the dose of 10, 30 and 60 mg/kg, respectively^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

765.44

Formula

C₄₂H₅₇ClN₄O₅S

CAS 号

2245848-05-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Wang H, et, al. Targeting MCL-1 in cancer: current status and perspectives. J Hematol Oncol. 2021 Apr 21;14(1):67.

[2]. Caenepeel S, et al. Abstract 6218: discovery and preclinical evaluation of AMG 397, a potent, selective and orally bioavailable MCL1 inhibitor. Cancer Res. 2020;80(16 Supplement):6218.

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AMG-Tie2-1

发表于2024年1月20日由上海金畔生物科技有限公司

AMG-Tie2-1

AMG-Tie2-1 是一种内膜内皮细胞激酶 2 (Tie2) 抑制剂，IC₅₀ 为 1 nM。AMG-Tie2-1 是一种 VEGFR2 抑制剂，IC₅₀ 为 3 nM。

AMG-Tie2-1 Chemical Structure

CAS No. : 870223-96-4

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生物活性	AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) with an IC₅₀ of 1 nM. AMG-Tie2-1 is a VEGFR2 inhibitor with an IC₅₀ of 3 nM^[1].
体外研究 (In Vitro)	AMG-Tie2-1 (compound 15) inhibits Tie-2 phosphorylation in EA.hy926 human endothelial cells (IC₅₀=10 nM). Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	479.45
Formula	C₂₅H₂₀F₃N₅O₂
CAS 号	870223-96-4
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Brian L Hodous, et al. Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor. J Med Chem. 2007 Feb 22;50(4):611-26.

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AMG-Tie2-1

发表于2024年1月20日由上海金畔生物科技有限公司

AMG-Tie2-1

AMG-Tie2-1 是一种内膜内皮细胞激酶 2 (Tie2) 抑制剂，IC₅₀ 为 1 nM。AMG-Tie2-1 是一种 VEGFR2 抑制剂，IC₅₀ 为 3 nM。

AMG-Tie2-1 Chemical Structure

CAS No. : 870223-96-4

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生物活性	AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) with an IC₅₀ of 1 nM. AMG-Tie2-1 is a VEGFR2 inhibitor with an IC₅₀ of 3 nM^[1].
体外研究 (In Vitro)	AMG-Tie2-1 (compound 15) inhibits Tie-2 phosphorylation in EA.hy926 human endothelial cells (IC₅₀=10 nM). 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	479.45
Formula	C₂₅H₂₀F₃N₅O₂
CAS 号	870223-96-4
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Brian L Hodous, et al. Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor. J Med Chem. 2007 Feb 22;50(4):611-26.

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AMG-Tie2-1

发表于2024年1月20日由上海金畔生物科技有限公司

AMG-Tie2-1

AMG-Tie2-1 是一种内膜内皮细胞激酶 2 (Tie2) 抑制剂，IC₅₀ 为 1 nM。AMG-Tie2-1 是一种 VEGFR2 抑制剂，IC₅₀ 为 3 nM。

AMG-Tie2-1 Chemical Structure

CAS No. : 870223-96-4

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生物活性	AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) with an IC₅₀ of 1 nM. AMG-Tie2-1 is a VEGFR2 inhibitor with an IC₅₀ of 3 nM^[1].
体外研究 (In Vitro)	AMG-Tie2-1 (compound 15) inhibits Tie-2 phosphorylation in EA.hy926 human endothelial cells (IC₅₀=10 nM). Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	479.45
Formula	C₂₅H₂₀F₃N₅O₂
CAS 号	870223-96-4
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Brian L Hodous, et al. Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor. J Med Chem. 2007 Feb 22;50(4):611-26.

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(±)-AMG 487

发表于2024年1月18日由上海金畔生物科技有限公司

(±)-AMG 487

(±)-AMG 487 是 AMG 487 的外消旋体。AMG 487 是一种有效的，具有口服活性的选择性趋化因子受体3 (CXCR3) 拮抗剂，抑制 CXCL10 和 CXCL11 与 CXCR3 结合的 IC₅₀ 值分别为 8.0 和 8.2 nM。

(±)-AMG 487 Chemical Structure

CAS No. : 947536-03-0

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生物活性	(±)-AMG 487 is a racemate of AMG 487. AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC₅₀s of 8.0 and 8.2 nM, respectively^[1].
分子量	603.59
Formula	C₃₂H₂₈F₃N₅O₄
CAS 号	947536-03-0
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Johnson M, et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43.

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(±)-AMG 487

发表于2024年1月18日由上海金畔生物科技有限公司

(±)-AMG 487

(±)-AMG 487 Chemical Structure

CAS No. : 947536-03-0

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生物活性	(±)-AMG 487 is a racemate of AMG 487. AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC₅₀s of 8.0 and 8.2 nM, respectively^[1].
分子量	603.59
Formula	C₃₂H₂₈F₃N₅O₄
CAS 号	947536-03-0
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Johnson M, et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43.

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(±)-AMG 487

发表于2024年1月18日由上海金畔生物科技有限公司

(±)-AMG 487

(±)-AMG 487 Chemical Structure

CAS No. : 947536-03-0

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生物活性	(±)-AMG 487 is a racemate of AMG 487. AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC₅₀s of 8.0 and 8.2 nM, respectively^[1].
分子量	603.59
Formula	C₃₂H₂₈F₃N₅O₄
CAS 号	947536-03-0
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Johnson M, et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43.

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AMG 900

发表于2023年11月3日由上海金畔生物科技有限公司

AMG 900 纯度: 99.29%

AMG 900 是一种有效的选择性的 pan-Aurora 激酶抑制剂，作用于 Aurora A，B 和 C，IC₅₀ 分别为 5 nM，4 nM 和 1 nM。

AMG 900 Chemical Structure

CAS No. : 945595-80-2

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生物活性

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC₅₀ of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.

IC₅₀ & Target^[1]

Aurora A

5 nM (IC₅₀)

Aurora B

4 nM (IC₅₀)

Aurora C

1 nM (IC₅₀)

体外研究
(In Vitro)

AMG 900 inhibits the enzyme activity of all 3 aurora kinase family members with IC₅₀ values of 5 nM or less. In HeLa cells, AMG 900 inhibits autophosphorylation of aurora-A and -B in a concentration-dependent manner. Treatment of HCT116 cells with 50 nM of AMG 900 for 48 hours resulted in polyploidy and suppresses the formation of colonies after cell replating. AMG 900 inhibits cell proliferation, with EC₅₀ values ranging from 0.7 to 5.3 nM. Importantly, 4 of these AMG 900-sensitive cell lines (HCT-15, MES-SA-Dx5, 769P, and SNU449) are resistant to paclitaxel and other anticancer agents. AMG 900 inhibits p-histone H3 or induced polyploidy across all the cell lines tested irrespective of P-gp or BCRP status with uniform potency (IC₅₀ or EC₅₀ values ranging from 2 to 3 nM)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

AMG 900 exhibits significant antitumor activity in all 9 xenograft models tested (50%-97% TGI compared with the vehicle-treated control group, P<0.005, P<0.0005). Importantly, AMG 900 is active in the MES-SA-Dx5 (84% TGI, P<0.0001) and NCI-H460-PTX (66% TGI, P<0.0001) xenograft models that are resistant to either Docetaxel or Paclitaxel administered at their respective maximum tolerated doses. AMG 900 inhibits the activity of aurora-B in HCT116 tumors and suppresses the growth of multiple xenografts that represent diverse tumor types^[1]. Treatment with AMG 900 at 15 mg/kg significantly inhibits p-Histone H3 in the G₂M cell population in mouse bone marrow (upper panel) and cytokeratin positive COLO 205 tumor (lower panel) compared with vehicle-treated controls^[2]. AMG 900 exhibits a low-to-moderate clearance and a small volume of distribution. Its terminal elimination half-life ranged from 0.6 to 2.4 h. AMG 900 is well-absorbed in fasted animals with an oral bioavailability of 31% to 107%. Food intake had an effect on rate (rats) or extent (dogs) of AMG 900 oral absorption^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

503.58

Formula

C₂₈H₂₁N₇OS

CAS 号

945595-80-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 50 mg/mL (99.29 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9858 mL	9.9289 mL	19.8578 mL
5 mM	0.3972 mL	1.9858 mL	3.9716 mL
10 mM	0.1986 mL	0.9929 mL	1.9858 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 5 mg/mL (9.93 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.93 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 5 mg/mL (9.93 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.93 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Payton M, et al. Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res, 2010, 70(23), 9846-9854.

[2]. Juan G, et al. AMG 900, a potent inhibitor of aurora kinases causes pharmacodynamic changes in p-Histone H3 immunoreactivity in human tumor xenografts and proliferating mouse tissues. J Transl Med. 2014 Nov 4;12:307.

[3]. Huang L, et al. In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases. Xenobiotica. 2011 May;41(5):400-8.

Cell Assay ^[1]	Different tumor cell lines including NCI-H460, MDA-MB231, MES-SA, NCI-H460 PTX, MDA-MB-231 PTX, MES-SA Dx5, and HCT-15. are treated with AMG 900 (0.5, 5.0, 50 nM) for 48 hours, washed twice with complete media, and cells are replated at a density of 5000 cells per well in drug-free complete media. Cells are grown until the DMSO control wells are confluent. Cells are stained with crystal violet dye, washed with distilled water, and imaged using a digital scanner^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]^[3]	Mice^[2] Female athymic nude mice of approximately 14 weeks of age are used. Mice are injected subcutaneously with 2×10⁶ COLO 205 cells in 100 μL of 50% matrigel. Mice with established tumors (approximately 200 mm³) are assigned into experimental groups (n=10 per group) and administered a single oral dose of vehicle or AMG 900 at 3.75, 7.5, and 15 mg/kg. Three hours after treatment tissue specimens (bone marrow, tumor, and skin) are collected from individual mice for pharmacodynamic and histological analysis. Blood plasma samples (50 μL) are collected from individual mice to determine the concentration of AMG 900 using quantitative methods. Excised tumors are divided in half for parallel flow and imaging based cytometric analyses. Rats^[3] Effect of food intake on AMG 900 PK is evaluated in male rats and male dogs following a single oral dose of AMG 900 at 5 mg/kg (rats) or 2 mg/kg (dogs) in the oral formulation mentioned above. For the rats, food is removed ~16 h before dosing for the fasted group, although the fed group had free access to standard laboratory rodent chow throughout the study; food is returned to rats in the fasted group 2 h post-dose. All the dogs are fasted for ~16 h before dosing. Each dog in the fed group receive 350 g of moist food 1 h prior to dosing, and any remaining food is removed after 1 h. All the dogs are fed 2 h post-dose. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Payton M, et al. Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res, 2010, 70(23), 9846-9854. [2]. Juan G, et al. AMG 900, a potent inhibitor of aurora kinases causes pharmacodynamic changes in p-Histone H3 immunoreactivity in human tumor xenografts and proliferating mouse tissues. J Transl Med. 2014 Nov 4;12:307. [3]. Huang L, et al. In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases. Xenobiotica. 2011 May;41(5):400-8.

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AMG 925 HCl

发表于2023年11月1日由上海金畔生物科技有限公司

AMG 925 HCl 纯度: 98.01%

AMG 925 HCl 是一种有效的选择性的 FLT3/CDK4 双重抑制剂，IC₅₀ 分别为 2±1 nM 和 3±1 nM。

AMG 925 HCl Chemical Structure

CAS No. : 1401034-19-2

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AMG 925 HCl 相关产品

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Bioactive Compound Library Plus

生物活性

AMG 925 HCl is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC₅₀s of 2±1 nM and 3±1 nM, respectively.

IC₅₀ & Target^[1]

FLT3

2 nM (IC₅₀)

CDK4

3 nM (IC₅₀)

CDK6

8 nM (IC₅₀)

CDK2

375 nM (IC₅₀)

CDK1

1.9 μM (IC₅₀)

体外研究
(In Vitro)

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

508.02

Formula

C₂₆H₃₀ClN₇O₂

CAS 号

1401034-19-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 1 mg/mL (1.97 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9684 mL	9.8421 mL	19.6843 mL
5 mM	—	—	—
10 mM	—	—	—

参考文献

[1]. Keegan K, et al. Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Mol Cancer Ther. 2014 Apr;13(4):880-9.

Cell Assay ^[1]	MOLM13 and Mv4-11 are used. MOLM13-Luc cells are constructed by transduction of MOLM13 cells with the pLV218G luciferin/lentivector, which expresses luciferase under the murine EF1α promoter. Sorafenib-resistant MOLM13 (MOLM13sr) and Mv4-11 (Mv4-11sr) are isolated by passaging the cells in growth medium containing increasing concentrations of Sorafenib (1-1 nM). Cell growth is measured by a DNA synthesis assay. Cells are seeded in a 96-well Cytostar T plate at a density of 5×10³ cells/well in a total volume of 160 μL. Test compounds (e.g., AMG 925; 0.03 and 0.3μM) are serially diluted into the plate (20 μL/well) and 20 μL/0.1 μCi of [¹⁴C]-Thymidine added to each well. Isotope incorporation is determined using a β plate counter after further 72-hour incubation. Apoptosis is assayed by using the Vybrant Apoptosis Assay Kit. Briefly, cells are seeded into a 6-well plate at 5×10⁵ cells per well and treated with compounds (e.g., AMG 925; 0.003, 0.01, 0.03, 0.1, 0.3, and 1 μM) for 24 hours. The cells are then stained with reagents provided in the kit and analyzed by flow cytometry. The Sytox Green fluorescence versus allophycocyanin fluorescence dot plot shows resolution of live, apoptotic, and dead cells, which are quantified using the Flowjo software. The cell-cycle analysis is done by treating the cells with AMG 925 for 24 hours followed by using the CycleTest Kit. Ten thousand events are acquired and the proportions of cells in each cycle phase are calculated using the ModFit software^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] *CrTac:NCR-Foxn1^nu* (NCR) nude mice are used. 2×10⁶ cells are innoculated on the flank of NCR nude mice and allowed to grow for 13 days. Mice are then dosed twice a day by oral administration 6 hours apart with 12.5, 25, 37.5, and 50 mg/kg of AMG 925 for 10 consecutive days^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.**
参考文献	[1]. Keegan K, et al. Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Mol Cancer Ther. 2014 Apr;13(4):880-9.

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Raleukin(Synonyms: 阿那白滞素; AMG-719)

发表于2023年10月30日由上海金畔生物科技有限公司

Raleukin (Synonyms: 阿那白滞素; AMG-719)

Raleukin (AMG-719) 是重组的、非溶酶化的 白细胞介素-1受体 (IL-1R) 的拮抗剂。Raleukin (AMG-719) 是第一个用于阻断促炎作用的生物制剂。

Raleukin Chemical Structure

CAS No. : 143090-92-0

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Bioactive Compound Library Plus

生物活性

Raleukin (AMG-719) is a recombinant, nonglycosylated human interleukin-1 receptor (IL-1R) antagonist. Raleukin (AMG-719) is the first biological agent to block the pro-inflammatory effects^[1]^[2].

IC₅₀ & Target

IL-1R^[1].

体内研究
(In Vivo)

Combined Etanercept (5 mg/kg, ip) and Anakinra (100 mg/kg, ip. daily for 7 days) substantially improves marginal mass human islet engraftment in immunodeficient mice^[2].
Raleukin (AMG-719) enhances tumor growth inhibition in mice receiving peptide vaccination and β-(1-3),(1-6)-D-glucan^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

17257.60

Formula

C₇₅₉H₁₁₈₆N₂₀₈O₂₃₂S₁₀

CAS 号

143090-92-0

中文名称

阿那白滞素

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Cvetkovic RS, et al. Anakinra. BioDrugs. 2002;16(4):303-11; discussion 313-4.

[2]. McCall M, et al. Anakinra potentiates the protective effects of etanercept in transplantation of marginal mass human islets in immunodeficient mice. Am J Transplant. 2012 Feb;12(2):322-9.

[3]. Harnack U, et al. IL-1 receptor antagonist anakinra enhances tumour growth inhibition in mice receiving peptide vaccination and beta-(1-3),(1-6)-D-glucan. Anticancer Res. 2010 Oct;30(10):3959-65.

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Navtemadlin(Synonyms: AMG 232; KRT-232)

发表于2023年10月29日由上海金畔生物科技有限公司

Navtemadlin (Synonyms: AMG 232; KRT-232) 纯度: 99.43%

Navtemadlin (AMG 232) 是一种有效，选择性，可口服的 p53-MDM2 相互作用抑制剂，IC₅₀ 值为 0.6 nM，与 MDM2 结合的 K_d 为 0.045 nM。

Navtemadlin Chemical Structure

CAS No. : 1352066-68-2

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5 mg	￥1800	In-stock
10 mg	￥2800	In-stock
25 mg	￥6000	In-stock
50 mg	￥10500	In-stock
100 mg	￥16500	In-stock
200 mg		询价
500 mg		询价

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Navtemadlin 相关产品

•相关化合物库:

Clinical Compound Library Plus
Bioactive Compound Library Plus
Peptidomimetic Library

生物活性

Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC₅₀ of 0.6 nM. Navtemadlin binds to MDM2 with a K_d of 0.045 nM^[1]^[2].

IC₅₀ & Target

IC50: 0.6 nM (p53-MDM2 interaction)^[1]
Kd: 0.045 nM (MDM2)^[1]

体外研究
(In Vitro)

Navtemadlin (AMG 232) (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines^[1].
Navtemadlin potently inhibits proliferation of non-MDM2-amplified HCT116 colorectal cells (IC₅₀=10 nM)^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347 and A427 cells.
Concentration:	0-10 μM.
Incubation Time:	72 hours.
Result:	Induced p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines (SJSA-1, HCT116, and ACHN). Caused robust p21 mRNA induction between 9.76 and 34.9 fold with IC50 values ranging from 12.8 to 46.8 nM.

体内研究
(In Vivo)

Navtemadlin (AMG 232) (10, 25, 75 mg/kg, once daily, p.o.) activates p53 pathway activity in vivo^[1].
Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) potently inhibits growth of tumor xenografts in mice^[1].
Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) blocks DNA synthesis and induces apoptosis in vivo^[1].
Navtemadlin causes a dose-dependent tumor growth inhibition with an ED₅₀ of 16 mg/kg^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice (n=10/group) based cancer models^[1].
Dosage:	10, 25, 75 mg/kg.
Administration:	Once daily by oral gavage.
Result:	Resulted in significant tumor growth inhibition across all models. SJSA-1, an MDM2 amplified osteosarcoma model, was the most sensitive to AMG 232 treatment with an ED₅₀ of 9.1 mg/kg. In the highest dose group of 75 mg/kg, 10/10 tumors completely regressed and were undetectable after 10 days of treatment.

Clinical Trial

分子量

568.55

Formula

C₂₈H₃₅Cl₂NO₅S

CAS 号

1352066-68-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

溶解性数据

In Vitro:

DMSO : ≥ 50 mg/mL (87.94 mM)

H₂O : ≥ 0.1 mg/mL (0.18 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7589 mL	8.7943 mL	17.5886 mL
5 mM	0.3518 mL	1.7589 mL	3.5177 mL
10 mM	0.1759 mL	0.8794 mL	1.7589 mL

请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 50% PEG300 50% saline

Solubility: 10 mg/mL (17.59 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.40 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline

Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution
5.

请依序添加每种溶剂： PBS

Solubility: 1.5 mg/mL (2.64 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Canon J, et al. The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents. Mol Cancer Ther. 2015 Mar;14(3):649-58.

[2]. Rew Y, et al. Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer. J Med Chem. 2014 Aug 14;57(15):6332-41.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Motesanib(Synonyms: 莫替沙尼; AMG 706)

发表于2023年10月28日由上海金畔生物科技有限公司

Motesanib (Synonyms: 莫替沙尼; AMG 706) 纯度: 99.99%

Motesanib (AMG 706) 是一种有效的 VEGFR1/2/3 的 ATP 竞争性抑制剂，IC₅₀ 值为 2 nM/3 nM/6 nM，与对 Kit 的选择性相似，是 PDGFR 和 Ret 的 10 倍多。

Motesanib Chemical Structure

CAS No. : 453562-69-1

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Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1210	In-stock
5 mg	￥1100	In-stock
10 mg	￥1900	In-stock
50 mg	￥5900	In-stock
100 mg	￥9500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Motesanib 相关产品

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Reprogramming Compound Library
Anti-Breast Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

Motesanib (AMG 706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC₅₀s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.

IC₅₀ & Target^[1]

VEGFR1

2 nM (IC₅₀)

VEGFR2

3 nM (IC₅₀)

VEGFR3

6 nM (IC₅₀)

体外研究
(In Vitro)

Motesanib has broad activity against the human VEGFR family, and displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC₅₀ of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC₅₀ of >3,000 nM. Motesanib also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC₅₀ of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells^[1]. Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib treatment significantly sensitizes the cells to fractionated radiation^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Motesanib (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED₅₀ of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells^[1]. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models^[2]. Motesanib treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

373.45

Formula

C₂₂H₂₃N₅O

CAS 号

453562-69-1

中文名称

莫替沙尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (267.77 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6777 mL	13.3887 mL	26.7773 mL
5 mM	0.5355 mL	2.6777 mL	5.3555 mL
10 mM	0.2678 mL	1.3389 mL	2.6777 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.69 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.69 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Polverino A, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer R

[2]. Kruser TJ, et al. Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin Cancer Res, 2010, 16(14), 3639-3647.

[3]. Coxon A, et al. Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors. Clin Cancer Res, 2009, 15(1), 110-118.

Kinase Assay ^[1]	Optimal enzyme, ATP, and substrate (gastrin peptide) concentrations are established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib is tested in a 10-point dose-response curve for each enzyme using an ATP concentration of two-thirds K_m for each. Most assays consist of enzyme mixed with kinase reaction buffer [20 mM Tris-HCl (pH 7.5), 10 mM MgCl₂, 5 mM MnCl₂, 100 mM NaCl, 1.5 mM EGTA]. A final concentration of 1 mM DTT, 0.2 mM NaVO₄, and 20 μg/mL BSA is added before each assay. For all assays, 5.75 mg/mL streptavidin-allophycocyanin and 0.1125 nM Eu-PT66 are added immediately before the HTRF reaction. Plates are incubated for 30 minutes at room temperature and read on a Discovery instrument. IC₅₀ values are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equation. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are preincubated for 2 hours with different concentrations of Motesanib, and exposed with 50 ng/mL VEGF or 20 ng/mL bFGF for an additional 72 hours. Cells are washed twice with DPBS, and plates are frozen at -70°C for 24 hours. Proliferation is assessed by the addition of CyQuant dye, and plates are read on a Victor 1420 workstation. IC₅₀ data are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equatio. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	A431 cells are cultured in DMEM (low glucose) with 10% FBS and penicillin/streptomycin/glutamine. Cells are harvested by trypsinization, washed, and adjusted to a concentration of 5×10⁷/mL in serum-free medium. Animals are challenged s.c. with 1×10⁷ cells in 0.2 mL over the left flank. Approximately 10 days thereafter, mice are randomized based on initial tumor volume measurements and treated with either vehicle (Ora-Plus) or Motesanib. Tumor volumes and body weights are recorded twice weekly and/or on the day of sacrifice. Tumor volume is measured with a Pro-Max electronic digital caliper and calculated using the formula length (mm)×width (mm)×height (mm) and expressed in mm³. Data are expressed as mean±SE. Repeated measures ANOVA followed by Scheffe post hoc testing for multiple comparisons is used to evaluate the statistical significance of observed differences. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Polverino A, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer R [2]. Kruser TJ, et al. Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin Cancer Res, 2010, 16(14), 3639-3647. [3]. Coxon A, et al. Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors. Clin Cancer Res, 2009, 15(1), 110-118.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

AMG 487

发表于2023年10月11日由上海金畔生物科技有限公司

AMG 487 纯度: 99.51%

AMG 487 是一种有效的、具有口服活性的、选择性的趋化因子受体3 (CXCR3) 拮抗剂，抑制 CXCL10和 CXCL11与 CXCR3 结合的 IC₅₀ 值分别为 8.0 和 8.2 nM。

AMG 487 Chemical Structure

CAS No. : 473719-41-4

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1912	In-stock
2 mg	￥1100	In-stock
5 mg	￥1440	In-stock
10 mg	￥2040	In-stock
50 mg	￥7680	In-stock
100 mg	￥11760	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

AMG 487 相关产品

•相关化合物库:

Bioactive Compound Library Plus
GPCR/G Protein Compound Library
Immunology/Inflammation Compound Library
Anti-Cancer Compound Library
Small Molecule Immuno-Oncology Compound Library
Endocrinology Compound Library
Orally Active Compound Library

生物活性

AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC₅₀s of 8.0 and 8.2 nM, respectively^[1].

IC₅₀ & Target^[1]

¹²⁵I-IP10-CXCR3

8 nM (IC₅₀)

¹²⁵I-ITAC-CXCR3

8.2 nM (IC₅₀)

体外研究
(In Vitro)

AMG 487 inhibits CXCR3-mediated cell migration by the three CXCR3 chemokines (IP-10 IC₅₀=8 nM, ITAC IC₅₀=15 nM, and MIG IC₅₀=36 nM). Furthermore, AMG 487 inhibits calcium mobilization in response to ITAC (IC₅₀=5 nM)^[1]. AMG487 (1 μM) develops into fewer lung metastases, and the lungs are significantly smaller than vehicle-treated lungs^[2]. AMG487 abrogates proliferation/survival of C26 tumour cells^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

AMG 487 (0.03-10 mg/kg, s.c.) exhibits significant reduction in cellular infiltration into the lungs in a dose dependent manner^[1]. AMG487 (5 mg/kg, s.c., twice daily) develops fewer metastases than that in vehicle-treated mice^[2]. AMG487 (5 mg/kg, s.c.)-treated mice exhibits fewer pulmonary nodules than the control mice in both the models. AMG487 reduces the tumour volume^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

603.59

Formula

C₃₂H₂₈F₃N₅O₄

CAS 号

473719-41-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 41 mg/mL (67.93 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6568 mL	8.2838 mL	16.5675 mL
5 mM	0.3314 mL	1.6568 mL	3.3135 mL
10 mM	0.1657 mL	0.8284 mL	1.6568 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 20% HP-β-CD in saline

Solubility: 5 mg/mL (8.28 mM); Suspened solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.14 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (4.14 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.14 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.14 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Johnson M, et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43.

[2]. Walser TC, et al. Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer Res. 2006 Aug 1;66(15):7701-7.

[3]. Cambien B, et al. Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism. Br J Cancer. 2009 Jun 2;100(11):1755-64.

Cell Assay ^[3]	Colon cancer cells are seeded at a density of 10⁴ cells cm² and incubated either in serum-enriched medium or in base medium (containing 0.1% bovine serum albumin, BSA) supplemented or not with various concentrations of rCXCL9, rCXCL10 and rCXCL11 for the indicated periods of time before being either trypsin-detached, collected and enumerated or re-fed with fresh medium for 3 days, harvested and enumerated. The morphology of the CRC cells is observed through an inverted optical microscope at ×20 magnification, and photographs are taken at day 7. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Local tumor growth and spontaneous metastasis are evaluated by injecting 3×10⁵ viable tumor cells s.c. proximal to the right abdominal mammary gland of syngeneic female mice. Tumor diameters are measured by caliper twice weekly, and mice are euthanized on an individual basis when the s.c. tumor measured 18 mm in diameter or earlier if the mouse seemed moribund. The lungs are removed and weighed, and surface tumor colonies are quantified in a blinded fashion under a dissecting microscope. Experimental metastasis is evaluated by injecting 9×10⁴ viable tumor cells i.v. into the lateral tail vein of syngeneic female mice. All mice are euthanized on day 21 posttransplantation or earlier if the mice seemed moribund. The lungs are removed and weighed, and surface tumor colonies are quantified in a blinded fashion under a dissecting microscope. A 50% hydroxypropyl-β-cyclodextrin solution is prepared; at 20%, this solution serves as the vehicle. AMG487 is added to the 50% solution, and it is incubated in a sonicating water bath for 2 hours with occasional vortexing. Distilled water is added to give the appropriate final concentration of AMG487 in 20% of hydroxypropyl-β-cyclodextrin. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Johnson M, et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. [2]. Walser TC, et al. Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer Res. 2006 Aug 1;66(15):7701-7. [3]. Cambien B, et al. Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism. Br J Cancer. 2009 Jun 2;100(11):1755-64.

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AMG-458

发表于2023年10月3日由上海金畔生物科技有限公司

AMG-458

AMG-458 是有效的、选择性的、具有口服活性的 c-Met 抑制剂，其对人和小鼠的 K_i 值分别为 1.2 nM 和 2.0 nM。

AMG-458 Chemical Structure

CAS No. : 913376-83-7

规格	价格	是否有货
5 mg	￥2100	询问价格 & 货期
10 mg	￥3100	询问价格 & 货期
25 mg	￥5900	询问价格 & 货期
50 mg	￥10500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性

AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with K_i values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively^[1].

IC₅₀ & Target^[1]

human c-Met

1.2 nM (Ki)

mouse c-Met

2.0 nM (Ki)

V1092I

1.1 nM (Ki)

D1228H

2.2 nM (Ki)

M1250T

4.1 nM (Ki)

H1094R

0.5 nM (Ki)

Y1230H

4.5 nM (Ki)

VEGDR2

4100 nM (Ki)

体内研究
(In Vivo)

AMG-458 (orally, 30, 100 mg/kg) significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NIH-3T3/TPR-Met model and U-87 MG human glioblastoma xenograft model^[1].
Dosage:	10, 30, 100 mg/kg.
Administration:	Orally q.d. or b.i.d.
Result:	With an ED₅₀ of ∼12 mg/kg and an ED₉₀ of ∼ 34 mg/kg in NIH-3T3/TPR-Met model. With an ED₅₀ of ∼16 mg/kg and an ED₉₀ of ∼ 59 mg/kg in U-87 MG human glioblastoma xenograft model. Significantly inhibited tumor growth at 30 and 100 mg/kg q.d. and 30 mg/kg b.i.d. without adverse effect on body weight.

Animal Model:	Balb/c mouse and SD rat^[1].
Dosage:	1 mg/kg (Pharmacokinetic Analysis).
Administration:	IV dose: 1 mg/kg (20% Captisol with pH adjusted to 3.5 using methanesulfonic acid).
Result:	Exhibited CL ((L/h)/kg) values of 0.16 and 0.73, V_ss (L/kg) values of 0.31 and 0.62, t_1/2 (h) values of 1.3 and 1.0 in mouse and rat, respectively.

分子量

539.58

Formula

C₃₀H₂₉N₅O₅

CAS 号

913376-83-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Longbin Liu, et al. Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). J Med Chem. 2008 Jul 10;51(13):3688-91.

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AMG 511

发表于2023年9月5日由上海金畔生物科技有限公司

AMG 511 纯度: 98.81%

AMG 511 是一个高效、口服有效的 I 类 pan-PI3K 抑制剂,对 PI3Kα, β, δ 和 γ 作用的 K_i 值分别为 4 nM, 6 nM, 2 nM 和 1 nM。AMG 511 减少 p-Akt (Ser473), 体现了它显著抑制了 PI3K 信号。AMG 511 在小鼠胶质母细胞瘤移植瘤模型中具有抗肿瘤活性。

AMG 511 Chemical Structure

CAS No. : 1253573-53-3

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2510	In-stock
5 mg	￥2200	In-stock
10 mg	￥4200	In-stock
25 mg	￥9400	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

AMG 511 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
PI3K/Akt/mTOR Compound Library
Stem Cell Signaling Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library
Anti-Aging Compound Library
Differentiation Inducing Compound Library
Oxygen Sensing Compound Library
Glycolysis Compound Library
Cytoskeleton Compound Library
Anti-Breast Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Anti-Cancer Metabolism Compound Library
Angiogenesis Related Compound Library
Glucose Metabolism Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with K_is of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model^[1].

IC₅₀ & Target

PI3Kα

4 nM (Ki)

PI3Kβ

6 nM (Ki)

PI3Kδ

2 nM (Ki)

PI3Kγ

1 nM (Ki)

体外研究
(In Vitro)

AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC₅₀ of 4 nM^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

AMG 511 potently blocks the targeted PI3K pathway in a mouse liver pharmacodynamic model (3-30 mg/kg; p.o.) and inhibits tumor growth in a U87 MG glioblastoma xenograft model (3-30 mg/kg; p.o.; daily; for 12 days)^[1].
AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female CD1 NU/NU mice, with U87 MG glioblastoma xenograft model^[1]
Dosage:	1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:	Oral administration, daily, for 12 days
Result:	Inhibited tumor growth.

Animal Model:	Male Sprague-Dawley rats^[1]
Dosage:	1 mg/kg
Administration:	Oral administration (Pharmacokinetic Analysis)
Result:	Had a superior pharmacokinetic profile with low clearance (0.4 L/h/kg, 12% of liver blood flow), good oral bioavailability (F = 60%), and a commensurate high oral exposure (AUC = 5.0 μM·h).

分子量

517.58

Formula

C₂₂H₂₈FN₉O₃S

CAS 号

1253573-53-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (64.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9321 mL	9.6603 mL	19.3207 mL
5 mM	0.3864 mL	1.9321 mL	3.8641 mL
10 mM	0.1932 mL	0.9660 mL	1.9321 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2 mg/mL (3.86 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (3.86 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Mark H Norman, et al. Selective Class I Phosphoinositide 3-kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511. J Med Chem. 2012 Sep 13;55(17):7796-816.

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Tapotoclax(Synonyms: AMG-176)

发表于2023年8月23日由上海金畔生物科技有限公司

Tapotoclax (Synonyms: AMG-176) 纯度: 99.80%

Tapotoclax (AMG-176) 是一种有效的、有口服活性的、骨髓细胞因子 1 (MCL-1) 的选择性抑制剂，其 K_i 值为 0.13 nM。

Tapotoclax Chemical Structure

CAS No. : 1883727-34-1

规格	价格	是否有货
1 mg	￥6800	In-stock
5 mg	￥19500	In-stock
10 mg		询价
50 mg		询价

* Please select Quantity before adding items.

Tapotoclax 相关产品

•相关化合物库:

Clinical Compound Library Plus
Bioactive Compound Library Plus
Macrocyclic Compound Library

生物活性

Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a K_i of 0.13 nM^[1]^[2].

IC₅₀ & Target^[1]

Mcl-1

0.13 nM (Ki)

体外研究
(In Vitro)

Tapotoclax is an inhibitor of induced myeloid leukemia cell differentiation protein MCL-1 (K_i=0.13 nM), with potential pro-apoptotic and antineoplastic activities. Upon administration, Tapotoclax binds to and inhibits the activity of MCL-1. This disrupts the formation of MCL-1/Bcl-2-like protein 11 (BCL2L11; BIM) complexes and induces apoptosis in tumor cells^[1]^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

613.21

Formula

C₃₃H₄₁ClN₂O₅S

CAS 号

1883727-34-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (101.92 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6308 mL	8.1538 mL	16.3076 mL
5 mM	0.3262 mL	1.6308 mL	3.2615 mL
10 mM	0.1631 mL	0.8154 mL	1.6308 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: 2 mg/mL (3.26 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (3.26 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2 mg/mL (3.26 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (3.26 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: 2 mg/mL (3.26 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (3.26 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Caenepeel S, et al. AMG 176, a Selective MCL1 Inhibitor, is Effective in Hematological Cancer Models Alone and in Combination with Established Therapies. Cancer Discov. 2018 Sep 25. pii: CD-18-0387.

[2]. Garner TP, et al. Progress in targeting the BCL-2 family of proteins. Curr Opin Chem Biol. 2017 Aug;39:133-142.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务