AZ12601011

发表于2024年4月14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。

AZ12601011 纯度: 99.25%

AZ12601011 是一种具有口服活性的，选择性 TGFBR1 激酶抑制剂，IC₅₀ 为 18 nM，K_d 为 2.9 nM。AZ12601011 通过选择性的抑制 ALK4，TGFBR1 和 ALK7 来抑制 SMAD2 的磷酸化。AZ12601011 抑制乳腺肿瘤的生长。

AZ12601011 Chemical Structure

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3850	In-stock
5 mg	￥3500	In-stock
10 mg	￥5800	In-stock
50 mg	￥15500	In-stock
100 mg	￥21500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

AZ12601011 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
TGF-beta/Smad Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Orally Active Compound Library
Anti-Pancreatic Cancer Compound Library
Angiogenesis Related Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library
Anti-Colorectal Cancer Compound Library

生物活性

AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC₅₀ of 18 nM and a K_d of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth ^[1].

IC₅₀ & Target^[1]

ALK4

ALK7

体外研究
(In Vitro)

AZ12601011 (0.01-10 μM; for 20 minutes) completely inhibits Phosphorylation of SMAD2 ^[1].
AZ12601011 (0.01 µM-10 µM) inhibits the activity of ALK4, ALK7 and TGFBR1 ^[1].
AZ12601011 inhibits 4T1 cells growth in vitro (IC₅₀=0.4µM) ^[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.

Western Blot Analysis^[1]

Cell Line:	NIH3T3, HaCaT, C2C12, T47D cells
Concentration:	0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
Incubation Time:	20 minutes
Result:	Completely inhibited Phosphorylation of SMAD2.

体内研究
(In Vivo)

AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo^[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 BALB/c mice at greater than 18g with tumour^[1]
Dosage:	50mg/kg
Administration:	Oral gavage; twice daily; for 25 days
Result:	Inhibited tumour growth and metastasis in vivo.

分子量

313.36

Formula

C₁₉H₁₅N₅

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 : 5 mg/mL (15.96 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1912 mL	15.9561 mL	31.9122 mL
5 mM	0.6382 mL	3.1912 mL	6.3824 mL
10 mM	0.3191 mL	1.5956 mL	3.1912 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。-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]. Spender LC, et al. Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor βSuperfamily Type 1 Receptors. Mol Pharmacol. 2019 Feb;95(2):222-234.

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

AZ-Dyrk1B-33

发表于2024年4月12日由上海金畔生物科技有限公司

AZ-Dyrk1B-33 纯度: 99.95%

AZ-Dyrk1B-33 是一种高效、选择性的 Dyrk1B 激酶抑制剂，其 IC₅₀ 值为 7 nM。

AZ-Dyrk1B-33 Chemical Structure

CAS No. : 1679330-37-0

规格	价格	是否有货
1 mg	￥1800	In-stock
5 mg	￥4800	In-stock
10 mg		询价
50 mg		询价

* Please select Quantity before adding items.

AZ-Dyrk1B-33 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

AZ-Dyrk1B-33 is a potent and selective Dyrk1B kinase inhibitor, with an IC₅₀ of 7 nM^[1].

IC₅₀ & Target

IC50: 7 nM (Dyrk1B)^[1]

体外研究
(In Vitro)

AZ-Dyrk1B-33 shows inhibition of phosphorylation of Dyrk pS421 in cells with an IC₅₀ of 0.192 μM^[1].
AZ-Dyrk1B-33 shows no effect in sensitization^[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

300.36

Formula

C₁₉H₁₆N₄

CAS 号

1679330-37-0

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:

DMSO : 125 mg/mL (416.17 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3293 mL	16.6467 mL	33.2934 mL
5 mM	0.6659 mL	3.3293 mL	6.6587 mL
10 mM	0.3329 mL	1.6647 mL	3.3293 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：

——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 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (6.93 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.93 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (6.93 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.93 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (6.93 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.93 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 20.8 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]. Kettle JG, et al. Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. J Med Chem. 2015 Mar 26;58(6):2834-44.

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

AZ505

发表于2024年4月11日由上海金畔生物科技有限公司

AZ505 纯度: 99.94%

AZ505 是一种有效的，具有选择性的 SMYD2 抑制剂，IC₅₀ 值为 0.12 μM。

AZ505 Chemical Structure

CAS No. : 1035227-43-0

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3113	In-stock
2 mg	￥1426	In-stock
5 mg	￥2450	In-stock
10 mg	￥4450	In-stock
25 mg	￥8900	In-stock
50 mg	￥12500	In-stock
100 mg	￥17500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

AZ505 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library

生物活性

AZ505 is a potent and selective SMYD2 inhibitor with an IC₅₀ of 0.12 μM.

IC₅₀ & Target

IC50: 0.12 μM (SMYD2)^[1]

体外研究
(In Vitro)

AZ505 is highly selective and shows an activity at submicromolar concentrations in vitro. The IC₅₀ of AZ505 for SMYD2 is 0.12 μM, which is >600-fold greater than the IC₅₀s of AZ505 for other histone methyltransferases, such as SMYD3 (IC₅₀>83.3 μM), DOT1L (IC₅₀>83.3 μM) and EZH2 (IC₅₀>83.3 μM)^[1]. AZ505 is a potent and selective SMYD2 inhibitor with an IC₅₀ of 0.12 μM. The human SMYD (SET and MYND domain-containing protein) family of protein lysine methyltransferases contains five members (SMYD1-5). Moreover, AZ505 fails to inhibit the enzymatic activities of a panel of protein lysine methyltransferases. AZ505 is nominated for ITC binding study with K_d of 0.5 μM. In contrast, the calculated K_d for the p53 substrate peptide is 3.7 μM. AZ505 binding to SMYD2 is driven primarily by entropy, which often suggests that binding is mediated by hydrophobic interactions with few specific hydrogen bonds^[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.

分子量

577.54

Formula

C₂₉H₃₈Cl₂N₄O₄

CAS 号

1035227-43-0

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:

DMSO : ≥ 42 mg/mL (72.72 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	1.7315 mL	8.6574 mL	17.3148 mL
5 mM	0.3463 mL	1.7315 mL	3.4630 mL
10 mM	0.1731 mL	0.8657 mL	1.7315 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: ≥ 2.25 mg/mL (3.90 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (3.90 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 22.5 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: ≥ 2.25 mg/mL (3.90 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (3.90 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 22.5 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: ≥ 2.25 mg/mL (3.90 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (3.90 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 22.5 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]. Komatsu S, et al. Overexpression of SMYD2 contributes to malignant outcome in gastric cancer. Br J Cancer. 2015 Jan 20;112(2):357-64.

[2]. Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73.

[3]. Li LX, et al. Lysine methyltransferase SMYD2 promotes cyst growth in autosomal dominant polycystic kidney disease. J Clin Invest. 2017 Jun 30;127(7):2751-2764.

Kinase Assay ^[2]	SMYD2 is expressed in insect cells and purified. AlphaScreen technology is used to screen our chemical library for small molecule inhibitors of SMYD2. Methylation (12 μL) reactions are carried out in TDT buffer (50 mM Tris-HCl [pH 9.0], 2 mM DTT, and 0.01% Tween 20) at room temperature using 1.25 nM SMYD2 protein, 200 nM SAM, and 100 nM biotinylated p53 peptide substrate (Biotin-aminohexanoyl-GSRAHSSHLKSKKGQSTSRH) in low volume 384-well plates. Following a 75 min incubation period, reactions are quenched by the addition of 5 μL of detection solution (20 mM HEPES [pH 7.4], 1.7 mg/mL BSA, 340 mM NaCl, 680 μM SAH, 0.04 mg/mL Streptavidin-coated AlphaScreen donor, and Protein A-coated acceptor beads), and 1 nM of a custom p53K370me1 polyclonal antibody. Reaction plates are incubated overnight in the dark at room temperature, and read using an Envision 2101 Multi-label Reader. Compounds showing >50% inhibition of SMYD2 are nominated for concentration dose-response determination, and are also subjected to an artifact assay. Seven compound concentrations are selected beginning at 30 μM with six half-log dilution steps. The artifact assay conditions are identical to those in the SMYD2 enzymatic activity assay, except for the absence of SMYD2 protein and the presence of 1 nM methylated p53 peptide. IC₅₀ values are calculated from dose-response data using in-house software^[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.
参考文献	[1]. Komatsu S, et al. Overexpression of SMYD2 contributes to malignant outcome in gastric cancer. Br J Cancer. 2015 Jan 20;112(2):357-64. [2]. Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73. [3]. Li LX, et al. Lysine methyltransferase SMYD2 promotes cyst growth in autosomal dominant polycystic kidney disease. J Clin Invest. 2017 Jun 30;127(7):2751-2764.

Kinase Assay
^[2]

SMYD2 is expressed in insect cells and purified. AlphaScreen technology is used to screen our chemical library for small molecule inhibitors of SMYD2. Methylation (12 μL) reactions are carried out in TDT buffer (50 mM Tris-HCl [pH 9.0], 2 mM DTT, and 0.01% Tween 20) at room temperature using 1.25 nM SMYD2 protein, 200 nM SAM, and 100 nM biotinylated p53 peptide substrate (Biotin-aminohexanoyl-GSRAHSSHLKSKKGQSTSRH) in low volume 384-well plates. Following a 75 min incubation period, reactions are quenched by the addition of 5 μL of detection solution (20 mM HEPES [pH 7.4], 1.7 mg/mL BSA, 340 mM NaCl, 680 μM SAH, 0.04 mg/mL Streptavidin-coated AlphaScreen donor, and Protein A-coated acceptor beads), and 1 nM of a custom p53K370me1 polyclonal antibody. Reaction plates are incubated overnight in the dark at room temperature, and read using an Envision 2101 Multi-label Reader. Compounds showing >50% inhibition of SMYD2 are nominated for concentration dose-response determination, and are also subjected to an artifact assay. Seven compound concentrations are selected beginning at 30 μM with six half-log dilution steps. The artifact assay conditions are identical to those in the SMYD2 enzymatic activity assay, except for the absence of SMYD2 protein and the presence of 1 nM methylated p53 peptide. IC₅₀ values are calculated from dose-response data using in-house software^[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.

参考文献

[1]. Komatsu S, et al. Overexpression of SMYD2 contributes to malignant outcome in gastric cancer. Br J Cancer. 2015 Jan 20;112(2):357-64.

[2]. Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73.

[3]. Li LX, et al. Lysine methyltransferase SMYD2 promotes cyst growth in autosomal dominant polycystic kidney disease. J Clin Invest. 2017 Jun 30;127(7):2751-2764.

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

AZ9482

发表于2024年3月11日由上海金畔生物科技有限公司

AZ9482 纯度: 98.17%

AZ9482 是 PARP1/2/6 的三重抑制剂，其对 PARP1/2/6 的IC₅₀ 值分别为 1 nM、1 nM 和640 nM。

AZ9482 Chemical Structure

CAS No. : 1825345-33-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1590	In-stock
1 mg	￥600	In-stock
5 mg	￥1600	In-stock
10 mg	￥2600	In-stock
25 mg	￥5000	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

AZ9482 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Epigenetics Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Anti-Breast Cancer Compound Library
Anti-Pancreatic Cancer Compound Library

生物活性

AZ9482 is a triple PARP1/2/6 inhibitor, with IC₅₀ values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively^[1].

体外研究
(In Vitro)

AZ9482 exhibits an EC₅₀ of 24 nM in MDA-MB-468 cells^[1].
AZ0108 treatment prevents CHK1 MARylation and induces hyperphosphorylation of CHK1, contributing to MPS formation and dysregulation of the cell cycle^[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.

Cell Viability Assay^[1]

Cell Line:	MDA-MB-468 cells.
Concentration:	0-10 μM.
Incubation Time:	3 days.
Result:	EC₅₀ was 24 nM.

体内研究
(In Vivo)

AZ0108 also displays toxicity in vivo, the molecular basis of which is currently undefined, limiting pharmacological evaluation of AZ0108^[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

450.49

Formula

C₂₆H₂₂N₆O₂

CAS 号

1825345-33-2

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 : 125 mg/mL (277.48 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2198 mL	11.0990 mL	22.1981 mL
5 mM	0.4440 mL	2.2198 mL	4.4396 mL
10 mM	0.2220 mL	1.1099 mL	2.2198 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: 2.08 mg/mL (4.62 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.62 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 20.8 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: 2.08 mg/mL (4.62 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.62 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 20.8 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: ≥ 2.08 mg/mL (4.62 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.62 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 20.8 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]. Ryan T Howard, et al. Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors. ACS Chem Biol. 2020 Feb 21;15(2):325-333.

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

AZ506

发表于2024年3月11日由上海金畔生物科技有限公司

AZ506 纯度: 99.74%

AZ506 是有效的 SMYD2 抑制剂，IC₅₀ 为 17 nM。AZ506 抑制细胞中 SMYD2 甲基转移酶的活性，导致 SMYD2 介导的甲基化信号减少。

AZ506 Chemical Structure

CAS No. : 2043321-54-4

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4720	In-stock
5 mg	￥4000	In-stock
10 mg	￥6800	In-stock
25 mg	￥13500	In-stock
50 mg	￥22000	In-stock
100 mg	￥34000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

AZ506 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Targeted Diversity Library

生物活性

AZ506 is a potent SMYD2 inhibitor with an IC₅₀ of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal^[1].

IC₅₀ & Target^[1]

SMYD2

17 nM (IC₅₀)

体外研究
(In Vitro)

AZ506 inhibits SMYD2 mediated methylation of monomethyl p53 peptide in U2OS cells with an EC₅₀ of 1.2 μM. AZ506 inhibits SMYD2-mediated methylation (p53-me in U2OS cells) with an IC₅₀ of 2.43 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.

分子量

536.71

Formula

C₃₃H₄₀N₆O

CAS 号

2043321-54-4

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 : 50 mg/mL (93.16 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8632 mL	9.3160 mL	18.6320 mL
5 mM	0.3726 mL	1.8632 mL	3.7264 mL
10 mM	0.1863 mL	0.9316 mL	1.8632 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 (4.66 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.66 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 (4.66 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.66 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.66 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]. Cowen SD, et al. Design, Synthesis, and Biological Activity of Substrate Competitive SMYD2 Inhibitors. J Med Chem. 2016;59(24):11079-11097.

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AZ12672857

发表于2024年3月7日由上海金畔生物科技有限公司

AZ12672857 纯度: 98.44%

AZ12672857 是具有口服活性的 EphB4 (IC₅₀=1.3 nM) 和 Src 激酶的抑制剂。AZ12672857 抑制 c-Src 转染 3T3 细胞的增殖 (IC₅₀=2 nM) 和抑制转染 CHO-K1 细胞中的 EphB4 自磷酸化 (IC₅₀=9 nM)。

AZ12672857 Chemical Structure

CAS No. : 945396-55-4

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4280	In-stock
5 mg	￥4000	In-stock
10 mg	￥6800	In-stock
25 mg	￥13500	In-stock
50 mg	￥22000	In-stock
100 mg	￥34000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

AZ12672857 相关产品

•相关化合物库:

Bioactive Compound Library Plus
GPCR/G Protein Compound Library
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
Anti-Cancer Compound Library
Orally Active Compound Library
Angiogenesis Related Compound Library
Targeted Diversity Library

生物活性

AZ12672857 is an orally active inhibitor of EphB4 (IC₅₀=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC₅₀=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC₅₀=9 nM)^[1].

IC₅₀ & Target^[1]

EP4

1.3 nM (IC₅₀)

Src

体外研究
(In Vitro)

AZ12672857 shows only modest inhibition of CYP P450 (IC₅₀=5 μM against 2C9 and 3A4, >10 μM against 1A4, 2D6 and 2C19). AZ12672857 inhibits p-KDR in HUVEC with an IC₅₀ of 240 nM and inhibits p-PDGFR-βin MG63 cell line with an IC₅₀ of 58 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.

分子量

486.57

Formula

C₂₆H₃₀N₈O₂

CAS 号

945396-55-4

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 : 25 mg/mL (51.38 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0552 mL	10.2760 mL	20.5520 mL
5 mM	0.4110 mL	2.0552 mL	4.1104 mL
10 mM	0.2055 mL	1.0276 mL	2.0552 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: ≥ 2.08 mg/mL (4.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.27 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.27 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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]. Bardelle C, et al. Inhibitors of the tyrosine kinase EphB4. Part 3: identification of non-benzodioxole-based kinase inhibitors. Bioorg Med Chem Lett. 2010;20(21):6242-6245.

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AZ304

发表于2024年3月4日由上海金畔生物科技有限公司

AZ304 纯度: 99.39%

AZ304 是一种 BRAF 双重抑制剂，有效抑制野生型 BRAF，突变型 BRAF (V600E) 和野生型 CRAF，IC₅₀ 值分别为 79 nM，38 nM 和 68 nM。AZ304 对其他激酶有显著抑制作用，如 p38 (IC₅₀，6 nM)，CSF1R (IC₅₀，35 nM)。具有抗肿瘤活性。

AZ304 Chemical Structure

CAS No. : 942507-42-8

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1650	In-stock
25 mg	￥1500	In-stock
50 mg	￥2500	In-stock
100 mg	￥4500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

AZ304 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
MAPK Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library
Oxygen Sensing Compound Library
Ferroptosis Compound Library
Glutamine Metabolism Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC₅₀s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC₅₀, 6 nM), CSF1R (IC₅₀, 35 nM). Anti-tumor activity^[1].

IC₅₀ & Target

BRaf^V600E

38 nM (IC₅₀)

BRAF^WT

79 nM (IC₅₀)

CRAF

68 nM (IC₅₀)

p38

6 nM (IC₅₀)

CSF1R

35 nM (IC₅₀)

MAP3K7

6400 nM (IC₅₀)

CSK

7050 nM (IC₅₀)

体外研究
(In Vitro)

AZ304 (1 nM-100 μM) potently reduces ERK phosphorylation (p-ERK), with a mean EC₅₀ of 65 nM in the V600E mutant BRAF containing melanoma cell line A375, and EC₅₀s of 52 nM, 60 nM in the wild type BRAF melanoma cell line SK-MEL-31 with and without EGF^[1]. AZ304 also potently inhibits p-p38 in both BRAF genetic statuses cell lines^[1].
AZ304 (0, 0.1, 1, 10, 100 μM, 48 and 72 hours) dose-dependently inhibits the growth of RKO, HT-29, DiFi, and Caco-2, with GI₅₀s of 4.539 μM, 3.896 μM, 4.987 μM, 1.763 μM (48 hours) and 0.5032 μM, 0.3887 μM, 0.6354 μM, 0.3772 μM (72 hours), respectively^[1].
AZ304 (2 μM, 36 and 48 hours) decreases BRAF, p-ERK, p-AKT and p-mTOR levels, increases p-EGFR in both BRAF V600E mutant and BRAF wild type cells. AZ304 down-regulates p-EGFR, inhibits p-ERK, more potently suppresses BRAF, ERK, AKT and mTOR signalling pathways in combination with C225^[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.

Cell Proliferation Assay^[1]

Cell Line:	RKO, HT-29, DiFi, Caco-2 cells
Concentration:	0, 0.1, 1, 10, 100 μM
Incubation Time:	48, 72 hours
Result:	Dose-dependently inhibited the growth of V600E mutant BRAF cell lines (RKO, HT-29) and wild-type BRAF cell lines (DiFi, Caco-2).

分子量

451.52

Formula

C₂₇H₂₅N₅O₂

CAS 号

942507-42-8

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 : 125 mg/mL (276.84 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2147 mL	11.0737 mL	22.1474 mL
5 mM	0.4429 mL	2.2147 mL	4.4295 mL
10 mM	0.2215 mL	1.1074 mL	2.2147 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: ≥ 2.08 mg/mL (4.61 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.61 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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: 2.08 mg/mL (4.61 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.61 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 20.8 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: ≥ 2.08 mg/mL (4.61 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.61 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 20.8 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]. Ma R, et al. AZ304, a novel dual BRAF inhibitor, exerts anti-tumour effects in colorectal cancer independently of BRAF genetic status. Br J Cancer. 2018 May;118(11):1453-1463.

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AZ14145845

发表于2023年12月18日由上海金畔生物科技有限公司

AZ14145845

AZ14145845 是一种具有体内药效的高选择性I1/2型Mer/Axl双特异性激酶抑制剂。

AZ14145845 Chemical Structure

规格	价格	是否有货
5 mg	￥3600	询问价格 & 货期
10 mg	￥5800	询问价格 & 货期
25 mg	￥11500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性	AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy.
分子量	561.68
Formula	C₃₂H₃₅N₉O
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]. McCoull W, et al. Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy. J Med Chem. 2021 Sep 23;64(18):13524-13539.

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AZ14145845

发表于2023年12月18日由上海金畔生物科技有限公司

AZ14145845

AZ14145845 是一种具有体内药效的高选择性I1/2型Mer/Axl双特异性激酶抑制剂。

AZ14145845 Chemical Structure

规格	价格	是否有货
5 mg	￥3600	询问价格 & 货期
10 mg	￥5800	询问价格 & 货期
25 mg	￥11500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性	AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy.
分子量	561.68
Formula	C₃₂H₃₅N₉O
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]. McCoull W, et al. Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy. J Med Chem. 2021 Sep 23;64(18):13524-13539.

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

AZ14145845

发表于2023年12月18日由上海金畔生物科技有限公司

AZ14145845

AZ14145845 是一种具有体内药效的高选择性I1/2型Mer/Axl双特异性激酶抑制剂。

AZ14145845 Chemical Structure

规格	价格	是否有货
5 mg	￥3600	询问价格 & 货期
10 mg	￥5800	询问价格 & 货期
25 mg	￥11500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性	AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy.
分子量	561.68
Formula	C₃₂H₃₅N₉O
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]. McCoull W, et al. Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy. J Med Chem. 2021 Sep 23;64(18):13524-13539.

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

AZ13705339

发表于2023年12月1日由上海金畔生物科技有限公司

AZ13705339

AZ13705339 是一种高效且具有选择性的 PAK1 抑制剂，对 PAK1 和 pPAK1 的 IC₅₀ 分别为 0.33 nM 和 59 nM。AZ13705339 对 PAK1 和 PAK2 具有结合亲和力，K_d 分别为 0.28 nM 和 0.32 nM。AZ13705339 在大鼠肝细胞中具有中等清除率 (CL_int = 30 µL/min/10^6)。

AZ13705339 Chemical Structure

CAS No. : 2016806-57-6

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

AZ13705339 is a highly potent and selective PAK1 inhibitor with IC₅₀s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 has binding affinities to PAK1 and PAK2, with K_ds of 0.28 nM and 0.32 nM, respectively. AZ13705339 has moderate clearance in rat hepatocytes (CL_int = 30 µL/min/10^6)^[1].

IC₅₀ & Target^[1]

PAK1

0.33 nM (IC₅₀)

PAK1

0.28 nM (Ki)

分子量

629.75

Formula

C₃₃H₃₆FN₇O₃S

CAS 号

2016806-57-6

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]. McCoull W, Hennessy EJ, Blades K, et al. Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. ACS Med Chem Lett. 2016;7(12):1118-1123. Published 2016 Sep 14.

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AZ5576

发表于2023年11月21日由上海金畔生物科技有限公司

AZ5576

AZ5576 是一种强效的高选择性 CDK9 抑制剂。AZ5576 可用于血液恶性肿瘤研究。

AZ5576 Chemical Structure

CAS No. : 2751721-40-9

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

AZ5576 is a potent and highly selective CDK9 inhibitor. AZ5576 can be used for hematological Malignancy research^[1].

IC₅₀ & Target^[1]

CDK9

分子量

385.43

Formula

C₂₁H₂₄FN₃O₃

CAS 号

2751721-40-9

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]. Bernard Barlaam, et al. Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.

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AZ5576

发表于2023年11月21日由上海金畔生物科技有限公司

AZ5576

AZ5576 是一种强效的高选择性 CDK9 抑制剂。AZ5576 可用于血液恶性肿瘤研究。

AZ5576 Chemical Structure

CAS No. : 2751721-40-9

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生物活性

AZ5576 is a potent and highly selective CDK9 inhibitor. AZ5576 can be used for hematological Malignancy research^[1].

IC₅₀ & Target^[1]

CDK9

分子量

385.43

Formula

C₂₁H₂₄FN₃O₃

CAS 号

2751721-40-9

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]. Bernard Barlaam, et al. Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.

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AZ5576

发表于2023年11月21日由上海金畔生物科技有限公司

AZ5576

AZ5576 是一种强效的高选择性 CDK9 抑制剂。AZ5576 可用于血液恶性肿瘤研究。

AZ5576 Chemical Structure

CAS No. : 2751721-40-9

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250 mg		询价
500 mg		询价

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生物活性

AZ5576 is a potent and highly selective CDK9 inhibitor. AZ5576 can be used for hematological Malignancy research^[1].

IC₅₀ & Target^[1]

CDK9

分子量

385.43

Formula

C₂₁H₂₄FN₃O₃

CAS 号

2751721-40-9

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]. Bernard Barlaam, et al. Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.

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Azido-PEG5-maleimide

发表于2023年11月13日由上海金畔生物科技有限公司

Azido-PEG5-maleimide

Azido-PEG5-maleimide 是一种 PROTAC linker，属于 PEG 类。可用于合成 PROTAC 分子。

Azido-PEG5-maleimide Chemical Structure

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生物活性

Azido-PEG5-maleimide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs^[1].

IC₅₀ & Target

PEGs

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins^[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

457.48

Formula

C₁₉H₃₁N₅O₈

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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.

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AZ12253801

发表于2023年11月7日由上海金畔生物科技有限公司

AZ12253801

AZ12253801 是一种 ATP 竞争性的 IGF-1R 酪氨酸激酶抑制剂。AZ12253801抑制 IGF-1R 驱动的 3T3 小鼠成纤维细胞(转染人IGF-1R)的增殖的 IC₅₀ 为17 nmol/L。抑制表皮生长因子受体(EGFR)诱导细胞增殖的 IC₅₀ 为440nmol/L。AZ12253801 具有抗肿瘤活性。

AZ12253801 Chemical Structure

CAS No. : 851432-37-6

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生物活性	AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC₅₀ of 17 nmol/L. The IC₅₀ for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.
分子量	402.45
Formula	C₂₁H₂₂N₈O
CAS 号	851432-37-6
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]. https://aacrjournals.org/cancerres/article/70/16/6412/559448/Type-1-Insulin-like-Growth-Factor-Receptor

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AZ-3

发表于2023年11月7日由上海金畔生物科技有限公司

AZ-3

AZ-3是有效，选择性的 JAK1 抑制剂，IC₅₀为34 nM。

AZ-3 Chemical Structure

CAS No. : 2228908-91-4

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生物活性	AZ-3 is a potent and selective JAK1 inhibitor with an IC₅₀ of 34 nM.
IC₅₀ & Target	IC50: 34 nM (JAK1)^[1]
分子量	385.48
Formula	C₂₀H₂₈FN₇
CAS 号	2228908-91-4
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]. Grimster NP, et al. Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors. J Med Chem. 2018 Jun 28;61(12):5235-5244.

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AZ1508(Synonyms: MC-Lys-MMETA)

发表于2023年11月3日由上海金畔生物科技有限公司

AZ1508 (Synonyms: MC-Lys-MMETA)

AZ1508 (MC-Lys-MMETA) 是一种用于 ADC 的药物-linker 偶联物 (drug-linker conjugates for ADC)，用于乳腺癌和胃癌的研究，其中药物是一种微管蛋白抑制剂。

AZ1508 Chemical Structure

CAS No. : 1817736-04-1

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生物活性	AZ1508 is a drug-linker conjugates for ADC for the treatment of breast and stomach cancer, and the drug is a tubulin inhibitor^[1].
分子量	1092.39
Formula	C₅₆H₈₅N₉O₁₁S
CAS 号	1817736-04-1
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]. Samantha Congreve, et al. Antibody drug conjugates (ADC) Current status and mapping of ADC:s in clinical programs. Uppsala Universitet.

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AZ3146

发表于2023年11月2日由上海金畔生物科技有限公司

AZ3146 纯度: 99.92%

AZ3146 是一种有效的选择性的 Mps1 抑制剂，作用于 Mps1^Cat，IC₅₀ 为 35 nM。

AZ3146 Chemical Structure

CAS No. : 1124329-14-1

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Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1216	In-stock
10 mg	￥1105	In-stock
50 mg	￥3464	In-stock
100 mg	￥5859	In-stock
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AZ3146 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Kinase Inhibitor Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Cytoskeleton Compound Library

生物活性

AZ3146 is a reasonably potent and selective Mps1 inhibitor with IC₅₀ of 35 nM for Mps1^Cat.

IC₅₀ & Target^[1]

Mps1^Cat

35 nM (IC₅₀)

体外研究
(In Vitro)

In in vitro kinase assays, AZ3146 inhibits human Mps1^Cat with IC₅₀ of ~35 nM. AZ3146 also efficiently inhibits autophosphorylation of full-length Mps1 immunoprecipitated from human cells^[1]. TTK specific kinase inhibitor AZ3146 can decrease HCC cell growth. In vitro cell cytotoxicity assays are performed on SMMC-7721 and BEL-7404 cells. IC₅₀s are calculated as being 7.13 μM (BEL-7404) and 28.62 μM (SMMC-7721). Both cells are further treated under the concentration of IC50 for 4 days. Significant inhibitions of cell proliferation are observed^[2]. HCT116 cells are cultured for 10 days in 0.8 μM (the GI₅₀) of AZ3146 , then 2 μM AZ3146 for 3 weeks. Sixteen clones are isolated and cell lines generated, named AzR1-16, all of which are resistant to AZ3146-induced cell death in cell viability assays; AzR3 and 4 have a GI₅₀ of approximately 3 μM (4-fold resistance), while the remaining clones have a GI₅₀ of approximately 9 μM (11-fold resistance). When analyzing mitosis by time-lapse microscopy, while 2 μM AZ3146 causes the parental cell line to rapidly exited mitosis in 10 minutes^[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

452.55

Formula

C₂₄H₃₂N₆O₃

CAS 号

1124329-14-1

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 : 100 mg/mL (220.97 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2097 mL	11.0485 mL	22.0970 mL
5 mM	0.4419 mL	2.2097 mL	4.4194 mL
10 mM	0.2210 mL	1.1049 mL	2.2097 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 (5.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.52 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 (5.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.52 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]. Hewitt L, et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J Cell Biol. 2010 Jul 12;190(1):25-34.

[2]. Liu X, et al. TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells. Oncotarget. 2015 Oct 27;6(33):34309-20.

[3]. Gurden MD, et al. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer Res. 2015 Aug 15;75(16):3340-54.

Kinase Assay ^[1]	His-tagged human Mps1^Cat encoding amino acids 510-857 is generated. For kinase assays, 500 ng is added to buffer (25 mM Tris-HCl, pH 7.4, 100 mM NaCl, 50 µg/mL BSA, 0.1 mM EGTA, 0.1% β-mercaptoethanol, 10 mM MgCl₂, and 0.5 µg/mL myelin basic protein), AZ3146, and 100 µM γ-[³²P]ATP (2 µCi/assay). Reactions are incubated at 30°C for 20 min, spotted onto P81 paper, washed in 0.5% phosphoric acid, and immersed in acetone. Phosphate incorporation is determined by scintillation counting. For immunoprecipitation kinase assays, HeLa cells are treated with nocodazole for 14 h, mitotic cells isolated, washed in PBS, and lysed for 30 min in 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 0.5% NP-40, 5 mM EDTA, 5 mM EGTA, 40 mM β-glycerophosphate, 0.2 mM PMSF, 1 mM DTT, 1 mM sodium orthovanadate, 20 mM sodium fluoride, 1 µM okadaic acid, and complete EDTA-free protease inhibitor cocktail. Full-length Mps1 is immunoprecipitated. Purified complexes are washed with lysis buffer containing 100 mM NaCl and assayed as described for the recombinant protein. To quantify ³²P incorporation, reactions are stopped with SDS sample buffer and separated by SDS-PAGE followed by phosphorimaging. The plate is analyzed using a phosphorimager using AIDA software. To assess the specificity of AZ3146, a single-point screen is carried using kinase profiling service. 50 kinases are selected and assayed with 1 µM AZ3146^[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.
Cell Assay ^[2]	The TTK inhibitor AZ3146 is disolved in DMSO at a concentration in 100 mM and diluted into 100 μM, 10 μM, 1 μM and 0.1 μM sequentially with DMEM containing 10% FBS before use. In vitrocytotoxicity assays are performed. HCC cells are plated into 96-well plates at the density of 3×10³ per well. AZ3146 is added in the indicated concentrations the next day. The inhibitor treated cells are cultured and tested at a 24-hour intervals for 3-4 days using CCK-8^[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.
参考文献	[1]. Hewitt L, et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J Cell Biol. 2010 Jul 12;190(1):25-34. [2]. Liu X, et al. TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells. Oncotarget. 2015 Oct 27;6(33):34309-20. [3]. Gurden MD, et al. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer Res. 2015 Aug 15;75(16):3340-54.

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AZ-5104

发表于2023年11月1日由上海金畔生物科技有限公司

AZ-5104 纯度: 99.70%

AZ-5104是AZD 9291的活性，去甲基化代谢物。AZ-5104是 EGFR 抑制剂；抑制EGFR^L858R/T790M，EGFR^L858R，EGFR^L861Q，EGFR 和ErbB4的 IC₅₀ 值分别为1，6，1，25和7 nM。

AZ-5104 Chemical Structure

CAS No. : 1421373-98-9

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Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥610	In-stock
5 mg	￥500	In-stock
10 mg	￥800	In-stock
50 mg	￥3000	In-stock
100 mg	￥4500	In-stock
200 mg	￥6000	In-stock
500 mg		询价
1 g		询价

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AZ-5104 相关产品

•相关化合物库:

Covalent Screening Library Plus
Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
JAK/STAT Compound Library
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Covalent Screening Library
Differentiation Inducing Compound Library
Anti-Hepatitis C Virus Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC₅₀s of 1, 6, 1, 25 and 7 nM for EGFR^L858R/T790M, EGFR^L858R, EGFR^L861Q, EGFR and ErbB4, respectively.

IC₅₀ & Target

EGFR^L858R/T790M

1 nM (IC₅₀)

EGFR^L858R

1 nM (IC₅₀)

EGFR^L861Q

6 nM (IC₅₀)

EGFR

25 nM (IC₅₀)

ErbB4

7 nM (IC₅₀)

EGFR^{Exon 19 deletion/T790M}

体外研究
(In Vitro)

AZ-5104 inhibits EGFR phosphorylation with IC₅₀s of 2, 1, 2, 53, and 33 nM in H1975 (EGFR^L858R/T790M), PC-9VanR (EGFR^{Exon 19 deletion/T790M}), PC-9 (EGFR^{Exon 19 deletion}), H2073 (WT), and LOVO (WT), respectively. AZ5104 exhibits a reduced selectivity margin against wild-type EGFR when compared to AZD9291. AZ5104 display minimal off-target activity against other non-HER family kinases, but has the potential to target both HER2 and HER4 kinase activity^[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)

The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice^[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

485.58

Formula

C₂₇H₃₁N₇O₂

CAS 号

1421373-98-9

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

溶解性数据

In Vitro:

DMSO : ≥ 28 mg/mL (57.66 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	2.0594 mL	10.2970 mL	20.5939 mL
5 mM	0.4119 mL	2.0594 mL	4.1188 mL
10 mM	0.2059 mL	1.0297 mL	2.0594 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 (5.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.15 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 (5.15 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.15 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.15 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]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61.

Cell Assay ^[1]	Cells were treated for 2 h with a dose-response of each drug (AZ-5104). Wild-type cells were stimulated for 10 minutes with 25 ng/mL of EGF before lysis. Level of EGFR phosphorylation was quantified in cell extracts using ELISA^[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]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61.

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