BMS-986299

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。

BMS-986299 纯度: 99.95%

BMS-986299 (compound 112) 是一流的 NLRP3 炎性小体激动剂，EC₅₀ 为 1.28 μM，来自专利 WO2018152396A1。

BMS-986299 Chemical Structure

CAS No. : 2242952-69-6

规格	价格	是否有货
5 mg	￥4800	In-stock
10 mg	￥8000	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

BMS-986299 相关产品

•相关化合物库:

Clinical Compound Library Plus
Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
NF-κB Signaling Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Antioxidants Compound Library
Oxygen Sensing Compound Library
Pyroptosis Compound Library

生物活性

BMS-986299 (compound 112) is a first-in-class NLRP3 inflammasome agonist with an EC₅₀ of 1.28 μM. (patent WO2018152396A1).

IC₅₀ & Target

NLRP3

1.28 μM (EC₅₀)

Clinical Trial

分子量

349.39

Formula

C₁₈H₁₉N₇O

CAS 号

2242952-69-6

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 (95.39 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8621 mL	14.3107 mL	28.6213 mL
5 mM	0.5724 mL	2.8621 mL	5.7243 mL
10 mM	0.2862 mL	1.4311 mL	2.8621 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。

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: ≥ 2.5 mg/mL (7.16 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.16 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 (7.16 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.16 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (7.16 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.16 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]. Gary Glick, et al. Substituted imidazo-quinolines as nlrp3 modulators. WO2018152396A1.

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Brivanib (alaninate)(Synonyms: BMS-582664)

发表于2024年4月10日由上海金畔生物科技有限公司

Brivanib (alaninate) (Synonyms: BMS-582664) 纯度: 99.45%

Brivanib alaninate (BMS-582664) 是一种 ATP 竞争性的 VEGFR2 抑制剂，IC₅₀ 值为 25 nM；可以适度抑制 VEGFR1 和 FGFR1，对 VEGFR2 的选择性是对 PDGFRβ 的 240 倍。

Brivanib (alaninate) Chemical Structure

CAS No. : 649735-63-7

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1540	In-stock
5 mg	￥1400	In-stock
10 mg	￥2550	In-stock
50 mg	￥7500	In-stock
100 mg	￥12600	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Brivanib (alaninate) 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Autophagy Compound Library
Drug Repurposing Compound Library
Differentiation Inducing Compound Library
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

Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC₅₀ of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ^[1].

IC₅₀ & Target^[1]

VEGFR2

25 nM (IC₅₀)

体外研究
(In Vitro)

Brivanib inhibits VEGFR1 and FGFR-1 with IC₅₀ of 0.38 μM and 0.148 μM. Brivanib is not sensitive to PDGFRβ, EGFR, LCK, PKCα or JAK-3 with IC₅₀ all above 1900 nM. Brivanib could inhibit the proliferation of VEGF-stimulated HUVECs with IC₅₀ of 40 nM, compared to 276 nM in FGF-stimulated HUVECs. On the other hand, brivanib exhibits low activity to tumor cell lines^[1]. Brivanib doses ≤20 µM paradoxically enhances FGF-induced LX-2 cell proliferation, whereas higher brivanib doses (≥30 µM) inhibits LX-2 cell proliferation. The inhibitory effect of brivanib on liver fibrosis is not through inhibition of TGF-β 1-induced stellate cell activation, and is possibly through inhibition of PDGF-BB-induced stellate cell activation^[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)

Brivanib displays antitumor activities in H3396 xenograft in athymic mice. At a dose of 60 and 90 mg/kg (p.o.), brivanib completely inhibits the tumor growth, with TGI of 85% and 97%, respectively^[1]. Moreover, brivanib significantly suppresses tumor growth in Hepatocellular carcinoma (HCC) xenografts, which due to the decrease in phosphorylation of VEGFR2. The results show that the tumor weights in 06-0606 xenograft mice are 55% and 13%, compared with the controls at a dose of 50 mg/kg and 100 mg/kg. Brivanib is suggested to be efficient in treatment of HCC^[2]. Brivanib (50 mg/kg, p.o.) attenuates liver fibrosis and stellate cell activation induced by BDL in mice. Brivanib inhibits growth factor and growth factor receptor mRNA expression in sham control animals but shows variable effects in bile duct ligated animals^[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

441.46

Formula

C₂₂H₂₄FN₅O₄

CAS 号

649735-63-7

中文名称

丙氨酸布立尼布

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 (226.52 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2652 mL	11.3261 mL	22.6521 mL
5 mM	0.4530 mL	2.2652 mL	4.5304 mL
10 mM	0.2265 mL	1.1326 mL	2.2652 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 (4.71 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.71 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 (4.71 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.71 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 (4.71 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.71 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]. Bhide RS, et al. Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J Med Chem, 2006, 49 (7), 2143-2146.

[2]. Nakamura I, et al. Correction: Brivanib Attenuates Hepatic Fibrosis In Vivo and Stellate Cell Activation In Vitro by Inhibition of FGF, VEGF and PDGF Signaling. PLoS One. 2015 Nov 3;10(11):e0142355.

[3]. Huynh H, et al. Brivanib alaninate, a dual inhibitor of vascular endothelial growth factor receptor and fibroblast growth factor receptor tyrosine kinases, induces growth inhibition in mouse models of human hepatocellular carcinoma. Clin Cancer Res, 2008, 14(19), 6146-6153.

Cell Assay ^[3]	Viability is measured in LX-2 cells using the Cell Counting Kit-8 (CCK-8). Using 96-well plates with 2,000 cells per well, HSCs are incubated in 10% FBS-supplemented DMEM for 24 hours, followed by starvation in serum-free media. After 24 hours of starvation, brivanib is added at different doses. Two hours later, 5 ng/mL PDGF-BB is added. The cells are incubated for an additional 72 hours and cell viability is measured. Each experiment is performed in three replicates at least four times^[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.
Animal Administration ^[3]	Male mice 4-6 weeks of age are treated 3 times a week with a total of 12 intraperitoneal (i.p.) injections of 150 mL/kg TAA. At the onset of TAA treatment, placebo or brivanib (25 or 50 mg/kg) is administered orally on 5 consecutive days with weekend breaks. The animals are sacrificed 4 weeks after the start of the injections^[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.
参考文献	[1]. Bhide RS, et al. Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J Med Chem, 2006, 49 (7), 2143-2146. [2]. Nakamura I, et al. Correction: Brivanib Attenuates Hepatic Fibrosis In Vivo and Stellate Cell Activation In Vitro by Inhibition of FGF, VEGF and PDGF Signaling. PLoS One. 2015 Nov 3;10(11):e0142355. [3]. Huynh H, et al. Brivanib alaninate, a dual inhibitor of vascular endothelial growth factor receptor and fibroblast growth factor receptor tyrosine kinases, induces growth inhibition in mouse models of human hepatocellular carcinoma. Clin Cancer Res, 2008, 14(19), 6146-6153.

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BMS-214662

发表于2024年4月9日由上海金畔生物科技有限公司

BMS-214662 纯度: 99.59%

BMS-214662是有效选择性的farnesyl transferase抑制剂，具有有效地抗肿瘤活性。

BMS-214662 Chemical Structure

CAS No. : 195987-41-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3770	In-stock
5 mg	￥3500	In-stock
10 mg	￥6000	In-stock
25 mg	￥12000	In-stock
50 mg	￥19500	In-stock
100 mg	￥34000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BMS-214662 相关产品

•相关化合物库:

Clinical Compound Library Plus
Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Anti-Pancreatic Cancer Compound Library

生物活性

BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC₅₀ of 1.35 nM.

IC₅₀ & Target

IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)^[1]

体外研究
(In Vitro)

BMS-214662 is over 1000-fold selective for farnesyl transferase, having IC₅₀ values for inhibition of geranylgeranylation of Ras-CVLL and K-Ras of 1.3 and 2.3 μM, respectively^[1]. BMS-214662 shows good potency in inhibiting H-ras-transformed rodent cells, A2780 human ovarian carcinoma tumor cells, and HCT-116 human colon carcinoma tumor cells. BMS-214662 is the most potent apoptotic FTI known and demonstrates broad spectrum yet robust cell-selective cytotoxic activity against a panel of cell lines with diverse histology^[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)

Tumors from BMS-214662-treated mice have increased numbers of apoptotic cells as compared with the nontreated control mice. The AIs in HCT-116 tumors are increased 4-10-fold in BMS-214662-treated mice as compared with nontreated controls. BMS-214662 is significantly cytotoxic to both HCT-116 and EJ-1 tumor cells; the doses of BMS-214662 required to kill 90% of clonogenic tumor cells are approximately 75 and 100 mg/kg for HCT-116 and EJ-1 tumors^[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

489.61

Formula

C₂₅H₂₃N₅O₂S₂

CAS 号

195987-41-8

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 : ≥ 100 mg/mL (204.24 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	2.0424 mL	10.2122 mL	20.4244 mL
5 mM	0.4085 mL	2.0424 mL	4.0849 mL
10 mM	0.2042 mL	1.0212 mL	2.0424 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 (5.11 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.11 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% corn oil

Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.11 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]. Hunt JT, et al. Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity. J Med Chem. 2000 Oct 5;43(20):3587-95.

[2]. Rose WC, et al. Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. Cancer Res. 2001 Oct 15;61(20):7507-17.

Cell Assay ^[2]	The hydrochloride salt of BMS-214662 is dissolved in DMSO with dilutions made using either water or RPMI 1640 plus 10% fetal bovine serum. BMS-214662 is added at various concentrations. The cells are incubated at 37°C for 72 h, at which time MTS in combination with phenazine methosulfate is added. After an additional 3 h, the absorbance is measured at 492 nm, and the growth inhibition results are eventually expressed as IC₅₀s^[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 Administration ^[2]	Mice: BMS-214662 is dissolved in ethanol, followed by dilution with water to a final ethanol concentration of 10%. Mice implanted with HCT-116 xenografts are administered a single dose of BMS-214662 at 250 mg/kg i.v., 300 mg/kg i.p., or 400 mg/kg p.o. An additional group receives 400 mg/kg BMS-214662 daily for 2 days (administered p.o. on day 1 and i.p. on day 2). Nontreated mice with time-matched HCT-116 tumors served as controls. Tumors are collected at 24 h after dose, processed following standard methods, sectioned, and stained with H&E. Serial sections of each tumor are processed for in situ apoptotic cell labeling by the TUNEL method^[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]. Hunt JT, et al. Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity. J Med Chem. 2000 Oct 5;43(20):3587-95. [2]. Rose WC, et al. Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. Cancer Res. 2001 Oct 15;61(20):7507-17.

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

生物活性分子抑制剂BMS-690514

发表于2024年4月8日由上海金畔生物科技有限公司

BMS-690514 纯度: 99.89%

BMS-690514是有效，有口服活性的 EGFR 和 VEGFR 的有效抑制剂，对于EGFR，HER2和HER4的IC₅₀ 值分别为5，9和60 nM。

BMS-690514 Chemical Structure

CAS No. : 859853-30-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1945	In-stock
2 mg	￥1600	In-stock
5 mg	￥2400	In-stock
10 mg	￥3580	In-stock
50 mg	￥9207	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

BMS-690514 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound 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
Clinical Compound Library
Drug Repurposing Compound Library
Differentiation Inducing Compound Library
Reprogramming Compound Library
Anti-Cardiovascular Disease Compound Library
Anti-COVID-19 Compound Library
Orally Active Compound Library
Anti-Hepatitis C Virus 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

BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC₅₀s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

IC₅₀ & Target^[1]

EGFR

5 nM (IC₅₀)

HER2

20 nM (IC₅₀)

HER4

60 nM (IC₅₀)

体外研究
(In Vitro)

BMS-690514 targets several critical signaling pathways: human epidermal growth factor receptor (HER)/ErbB, angiogenesis signaling through VEGFR2, lymphangiogenesis through VEGFR3, and also shows activity against VEGFR1, Flt-3, and Lck. Permeability of BMS-690514 in Caco-2 cells is in the intermediate range with a moderate potential to be a P-gp substrate^[2]. BMS-690514 inhibits members of the VEGFR family with IC₅₀ values in the range of 25 to 50 nM. Non–small cell lung tumor cells with exon 19 deletion (HCC4006, HCC827, and PC9) are highly sensitive to BMS-690514, which inhibits their proliferation with IC₅₀ values of 2 to 35 nM. Tumor cell lines with EGFR gene amplification (DiFi, NCI-H2073, A431) are also highly sensitive to inhibition by BMS-690514. Tumor cell lines that are dependent on HER2 signaling are also found to be highly sensitive to BMS-690514. Breast and gastric tumor cell lines that have HER2 gene amplification (N87, SNU-216, AU565, BT474, KPL4, and HCC202) are inhibited with IC₅₀ values of 20 to 60 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)

BMS-690514 has been shown to be efficacious in a broad spectrum of tumor xenografts. At doses that are efficacious and well tolerated in the animal models, BMS-690514 inhibits tumor cell proliferation and tumor blood flow^[1]. The oral bioavailability of BMS-690514 is 78% in mice, 100% in rats, 8% in monkeys, and 29% in dogs. BMS-690514 is able to cross the blood–brain barrier with a brain-to-plasma ratio of 1. The preclinical ADME properties of BMS-690514 suggest good oral bioavailability in humans and metabolism by multiple pathways including oxidation and glucuronidation^[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

368.43

Formula

C₁₉H₂₄N₆O₂

CAS 号

859853-30-8

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 : ≥ 25 mg/mL (67.86 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	2.7142 mL	13.5711 mL	27.1422 mL
5 mM	0.5428 mL	2.7142 mL	5.4284 mL
10 mM	0.2714 mL	1.3571 mL	2.7142 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 (6.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.79 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 (6.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.79 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.79 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]. Wong TW, et al. Antitumor and antiangiogenic activities of BMS-690514, an inhibitor of human EGF and VEGF receptor kinase families. Clin Cancer Res. 2011 Jun 15;17(12):4031-41.

[2]. Marathe P, et al. Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.

Animal Administration ^[2]	Rats: BMS-690514 is administered to male Sprague–Dawley rats as a 10 min infusion intraarterially (IA) (1 mg/kg) or orally by gavage (10mg/kg). Vehicles used for dosing are: IA, 10mM acetate buffer (pH 5.0, 1 mL/kg) and PO, PEG400/10mM acetate buffer (pH 5.0, 2 mL/kg) (10:90). Serial plasma samples are obtained predose and at 0.17 (or 0.25 for PO), 0.5, 0.75, 1, 2, 4, 6, 8, 12, and 24 h postdose. Rats are fasted overnight and fed 4 h postdose. The brain uptake of BMS-690514 is investigated after the last dose in a 2-week toxicology study (3, 10, and 30 mg/kg/day). Brain samples are weighed and homogenized in 3 volumes of ice-chilled water. Concentrations of BMS-690514 in plasma and brain homogenates are determined by LC/MS/MS^[2]. Mice: The pharmacokinetics of BMS-690514 is investigated in male balb-c mice. A total of 18 mice are divided into two groups to receive BMS-690514 as a single dose of 1mg/kg IV bolus or 5 mg/kg orally by gavage. The vehicle used for both IV (0.1mL/mouse) and PO (0.2mL/mouse) dose is Tween-80/PG/water (10:40:50). Serum concentrations of BMS-690514 are measured at 0.05 (or 0.25 for PO), 0.5, 1, 3, 6, 8, and 24 h postdose. The mice are fasted overnight and fed 6 h after dosing. Three blood samples are taken from each mouse by retro-orbital bleeding and there are three mice per time point. At the 24h time point only one sample is taken from each of the three mice. Composite serum concentration–time profiles are constructed for pharmacokinetic analysis^[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]. Wong TW, et al. Antitumor and antiangiogenic activities of BMS-690514, an inhibitor of human EGF and VEGF receptor kinase families. Clin Cancer Res. 2011 Jun 15;17(12):4031-41. [2]. Marathe P, et al. Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.

Animal Administration
^[2]

Rats: BMS-690514 is administered to male Sprague–Dawley rats as a 10 min infusion intraarterially (IA) (1 mg/kg) or orally by gavage (10mg/kg). Vehicles used for dosing are: IA, 10mM acetate buffer (pH 5.0, 1 mL/kg) and PO, PEG400/10mM acetate buffer (pH 5.0, 2 mL/kg) (10:90). Serial plasma samples are obtained predose and at 0.17 (or 0.25 for PO), 0.5, 0.75, 1, 2, 4, 6, 8, 12, and 24 h postdose. Rats are fasted overnight and fed 4 h postdose. The brain uptake of BMS-690514 is investigated after the last dose in a 2-week toxicology study (3, 10, and 30 mg/kg/day). Brain samples are weighed and homogenized in 3 volumes of ice-chilled water. Concentrations of BMS-690514 in plasma and brain homogenates are determined by LC/MS/MS^[2].

Mice: The pharmacokinetics of BMS-690514 is investigated in male balb-c mice. A total of 18 mice are divided into two groups to receive BMS-690514 as a single dose of 1mg/kg IV bolus or 5 mg/kg orally by gavage. The vehicle used for both IV (0.1mL/mouse) and PO (0.2mL/mouse) dose is Tween-80/PG/water (10:40:50). Serum concentrations of BMS-690514 are measured at 0.05 (or 0.25 for PO), 0.5, 1, 3, 6, 8, and 24 h postdose. The mice are fasted overnight and fed 6 h after dosing. Three blood samples are taken from each mouse by retro-orbital bleeding and there are three mice per time point. At the 24h time point only one sample is taken from each of the three mice. Composite serum concentration–time profiles are constructed for pharmacokinetic analysis^[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]. Wong TW, et al. Antitumor and antiangiogenic activities of BMS-690514, an inhibitor of human EGF and VEGF receptor kinase families. Clin Cancer Res. 2011 Jun 15;17(12):4031-41.

[2]. Marathe P, et al. Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.

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生物活性分子抑制剂BMS-690514

发表于2024年4月8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。
BMS-690514 纯度: 99.89%

BMS-690514是有效，有口服活性的 EGFR 和 VEGFR 的有效抑制剂，对于EGFR，HER2和HER4的IC₅₀ 值分别为5，9和60 nM。

BMS-690514 Chemical Structure

CAS No. : 859853-30-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1945	In-stock
2 mg	￥1600	In-stock
5 mg	￥2400	In-stock
10 mg	￥3580	In-stock
50 mg	￥9207	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

BMS-690514 相关产品

•相关化合物库:

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Anti-Blood Cancer Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC₅₀s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

IC₅₀ & Target^[1]

EGFR

5 nM (IC₅₀)

HER2

20 nM (IC₅₀)

HER4

60 nM (IC₅₀)

体外研究
(In Vitro)

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)

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

368.43

Formula

C₁₉H₂₄N₆O₂

CAS 号

859853-30-8

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 : ≥ 25 mg/mL (67.86 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	2.7142 mL	13.5711 mL	27.1422 mL
5 mM	0.5428 mL	2.7142 mL	5.4284 mL
10 mM	0.2714 mL	1.3571 mL	2.7142 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 (6.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.79 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 (6.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.79 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.79 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]. Wong TW, et al. Antitumor and antiangiogenic activities of BMS-690514, an inhibitor of human EGF and VEGF receptor kinase families. Clin Cancer Res. 2011 Jun 15;17(12):4031-41.

[2]. Marathe P, et al. Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.

Animal Administration ^[2]	Rats: BMS-690514 is administered to male Sprague–Dawley rats as a 10 min infusion intraarterially (IA) (1 mg/kg) or orally by gavage (10mg/kg). Vehicles used for dosing are: IA, 10mM acetate buffer (pH 5.0, 1 mL/kg) and PO, PEG400/10mM acetate buffer (pH 5.0, 2 mL/kg) (10:90). Serial plasma samples are obtained predose and at 0.17 (or 0.25 for PO), 0.5, 0.75, 1, 2, 4, 6, 8, 12, and 24 h postdose. Rats are fasted overnight and fed 4 h postdose. The brain uptake of BMS-690514 is investigated after the last dose in a 2-week toxicology study (3, 10, and 30 mg/kg/day). Brain samples are weighed and homogenized in 3 volumes of ice-chilled water. Concentrations of BMS-690514 in plasma and brain homogenates are determined by LC/MS/MS^[2]. Mice: The pharmacokinetics of BMS-690514 is investigated in male balb-c mice. A total of 18 mice are divided into two groups to receive BMS-690514 as a single dose of 1mg/kg IV bolus or 5 mg/kg orally by gavage. The vehicle used for both IV (0.1mL/mouse) and PO (0.2mL/mouse) dose is Tween-80/PG/water (10:40:50). Serum concentrations of BMS-690514 are measured at 0.05 (or 0.25 for PO), 0.5, 1, 3, 6, 8, and 24 h postdose. The mice are fasted overnight and fed 6 h after dosing. Three blood samples are taken from each mouse by retro-orbital bleeding and there are three mice per time point. At the 24h time point only one sample is taken from each of the three mice. Composite serum concentration–time profiles are constructed for pharmacokinetic analysis^[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]. Wong TW, et al. Antitumor and antiangiogenic activities of BMS-690514, an inhibitor of human EGF and VEGF receptor kinase families. Clin Cancer Res. 2011 Jun 15;17(12):4031-41. [2]. Marathe P, et al. Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.

Animal Administration
^[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]. Wong TW, et al. Antitumor and antiangiogenic activities of BMS-690514, an inhibitor of human EGF and VEGF receptor kinase families. Clin Cancer Res. 2011 Jun 15;17(12):4031-41.

[2]. Marathe P, et al. Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.

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

BMS453(Synonyms: BMS-189453)

发表于2024年3月16日由上海金畔生物科技有限公司

BMS453 (Synonyms: BMS-189453) 纯度: 98.89%

BMS453 (BMS-189453) 是一种合成类维生素 A，是一种 RARβ 激动剂和 RARα/RARγ 拮抗剂。BMS453 主要通过诱导活性 TGFβ 来抑制乳腺细胞生长。

BMS453 Chemical Structure

CAS No. : 166977-43-1

规格	价格	是否有货
5 mg	￥3200	In-stock
10 mg		询价
50 mg		询价

* Please select Quantity before adding items.

BMS453 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Transcription Factor Targeted Library

生物活性

BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ^[1]^[2].

体外研究
(In Vitro)

BMS453 (1 μM; 11 hours; 184 and HMEC cells) treatment inhibits the proliferation of normal breast cell growth without significantly inducing apoptosis^[2].
BMS453 (1 μM; 5 days; 184 and HMEC cells) treatment inhibits normal breast cell proliferation by causing G1 arrest^[2].
BMS453 (1 μM; 24-72 hours; 184 cells) treatment induces Rb hypophosphorylation and decrease CDK2 kinase activity. BMS453 increases total p21 protein levels and CDK2-bound p21 protein, but does not change CDK4-bound p21^[2].
BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ^[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.

Cell Proliferation Assay^[2]

Cell Line:	Normal human mammary epithelial cells (184 and HMEC)
Concentration:	1 μM
Incubation Time:	11 hours
Result:	Inhibited ³H-thymidine uptake in normal breast cells (184 and HMEC) by 40 %.

Cell Cycle Analysis^[2]

Cell Line:	Normal human mammary epithelial cells (184 and HMEC)
Concentration:	1 μM
Incubation Time:	5 days
Result:	Increased the proportion of cells in G0/G1 phase and decreased the proportion of cells in S phase.

Western Blot Analysis^[2]

Cell Line:	184 cells
Concentration:	1 μM
Incubation Time:	24 hours, 48 hours, 72 hours
Result:	Induced Rb hypophosphorylation and decrease CDK2 kinase activity.

分子量

380.48

Formula

C₂₇H₂₄O₂

CAS 号

166977-43-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

参考文献

[1]. J Y Chen, et al. RAR-specific agonist/antagonists which dissociate transactivation and AP1 transrepression inhibit anchorage-independent cell proliferation. EMBO J. 1995 Mar 15;14(6):1187-97.

[2]. L Yang, et al. The retinoic acid receptor antagonist, BMS453, inhibits normal breast cell growth by inducing active TGFbeta and causing cell cycle arrest. Oncogene. 2001 Nov 29;20(55):8025-35.

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

BMS-P5 free base

发表于2024年3月9日由上海金畔生物科技有限公司

BMS-P5 free base 纯度: 99.94%

BMS-P5 free base 是特异性的、具有口服活性的肽精氨酸二亚胺酶 4 (PAD4) 的抑制剂。BMS-P5 free base 可阻断多发性骨髓瘤诱导的 NET 形成，并延缓肿瘤进程。

BMS-P5 free base Chemical Structure

CAS No. : 1550371-22-6

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥5200	In-stock
5 mg	￥5000	In-stock
10 mg	￥8500	In-stock
25 mg		询价
50 mg		询价

* Please select Quantity before adding items.

BMS-P5 free base 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Anti-Cancer Compound Library
Orally Active Compound Library

生物活性

BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 free base blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model^[1].

体外研究
(In Vitro)

BMS-P5 blocks calcium ionophore-induced citrullination of histone H3^[1].
BMS-P5 is also able to inhibit formation of NETs induced by primary MM cells isolated from the BM of patients with MM^[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:	Neutrophils.
Concentration:	10 µM and 100 µM.
Incubation Time:	30 min followed by addition of DP42 or 5TGM1 CM.
Result:	Prevented MM-induced NET formation.

体内研究
(In Vivo)

BMS-P5 (50 mg/kg, oral gavage) significantly improves survival of MM-bearing mice^[1].
BMS-P5 (50 mg/kg, oral gavage) may attenuate the presence of pro-tumorigenic proteins in the tumor microenvironment, and thus delay tumor progression^[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:	Syngeneic mouse model of MM^[1].
Dosage:	50 mg/kg.
Administration:	Oral gavage, twice a day beginning on day 3 after tumor cell injection.
Result:	Significantly delayed development of symptoms and significantly prolonged survival of MM-bearing mice.

分子量

472.58

Formula

C₂₇H₃₂N₆O₂

CAS 号

1550371-22-6

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 : 250 mg/mL (529.01 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1160 mL	10.5802 mL	21.1604 mL
5 mM	0.4232 mL	2.1160 mL	4.2321 mL
10 mM	0.2116 mL	1.0580 mL	2.1160 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: ≥ 25 mg/mL (52.90 mM); Clear solution

此方案可获得 ≥ 25 mg/mL (52.90 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 250.0 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: ≥ 25 mg/mL (52.90 mM); Clear solution

此方案可获得 ≥ 25 mg/mL (52.90 mM，饱和度未知) 的澄清溶液。

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 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: ≥ 25 mg/mL (52.90 mM); Clear solution

此方案可获得 ≥ 25 mg/mL (52.90 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。

*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]. Marina Li, et al. A Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Mol Cancer Ther. 2020 Jul;19(7):1530-1538.

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BMS-983970

发表于2024年2月29日由上海金畔生物科技有限公司

BMS-983970 纯度: 99.42%

BMS-983970 是一种可口服的 Notch 抑制剂，具有抗肿瘤活性。

BMS-983970 Chemical Structure

CAS No. : 1584713-87-0

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3992	In-stock
2 mg	￥2333	In-stock
5 mg	￥3500	In-stock
10 mg	￥5000	In-stock
50 mg	￥15000	In-stock
100 mg	￥21000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BMS-983970 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Neuronal Signaling Compound Library
Stem Cell Signaling Compound Library
Wnt/Hedgehog/Notch Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Differentiation Inducing Compound Library
Anti-Breast Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Angiogenesis Related Compound Library
Transcription Factor Targeted Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

BMS-983970 is an oral pan-Notch inhibitor for the treatment of multiplecancers^[1].

IC₅₀ & Target

Notch^[1]

体内研究
(In Vivo)

BMS-983970 demonstrates anti-tumor activity in T-cell acute lymphoblastic leukemia (T-ALL) and solid tumor xenograft models^[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

518.50

Formula

C₂₆H₂₆F₄N₄O₃

CAS 号

1584713-87-0

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 : ≥ 50 mg/mL (96.43 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	1.9286 mL	9.6432 mL	19.2864 mL
5 mM	0.3857 mL	1.9286 mL	3.8573 mL
10 mM	0.1929 mL	0.9643 mL	1.9286 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 (4.82 mM); Suspended solution; Need ultrasonic and warming

此方案可获得 2.5 mg/mL (4.82 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 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 (4.82 mM); Suspended solution; Need ultrasonic and warming

此方案可获得 2.5 mg/mL (4.82 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 (4.82 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.82 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]. Ashvinikumar V. Gavai, et al. Abstract 1643: BMS-983970, an oral pan-Notch inhibitor for the treatment of cancer. Cancer Res October 1, 2014 74; 1643.

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SR11237(Synonyms: BMS-649)

发表于2024年2月23日由上海金畔生物科技有限公司

SR11237 (Synonyms: BMS-649) 纯度: 99.46%

SR11237 (BMS-649) 是一种视黄醇 X 受体 (RXR) 选择性激动剂，没有任何 RAR 活性。SR11237可导致 RXR/RXR 同型二聚体形成并激活含有 RXR 反应元件的报告基因。

SR11237 Chemical Structure

CAS No. : 146670-40-8

规格	价格	是否有货
5 mg	￥3000	In-stock
10 mg		询价
50 mg		询价

* Please select Quantity before adding items.

SR11237 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Differentiation Inducing Compound Library
Reprogramming Compound Library
Transcription Factor Targeted Library

生物活性

SR11237 (BMS-649) is a potent retinoid X receptor (RXR)-selective agonist that is devoid of any RAR activity. SR11237 can cause RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element^[1]^[2]^[3].

体外研究
(In Vitro)

Using nuclear receptor co-transfection assays in COS-1 cells, that SR11237 is effective at transactivating a chloramphenicol acetyltransferase reporter gene through RXRs but not retinoic acid receptors^[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)

SR11237 (BMS-649) (25 mg/kg; i.p.; daily from post-natal days 5 to 15) causes irregular ossification and premature closure of the growth plate^[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:	Sprague-Dawley rats^[2]
Dosage:	25 mg/kg
Administration:	I.p.; daily from post-natal days 5 to 15
Result:	Caused disturbed ossification and bone morphology in rats, including premature growth plate closure and infiltration of ossified tissue through the central epiphysis.

分子量

380.48

Formula

C₂₄H₂₈O₄

CAS 号

146670-40-8

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 : 5 mg/mL (13.14 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6283 mL	13.1413 mL	26.2826 mL
5 mM	0.5257 mL	2.6283 mL	5.2565 mL
10 mM	0.2628 mL	1.3141 mL	2.6283 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% corn oil

Solubility: ≥ 0.5 mg/mL (1.31 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.31 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 5.0 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]. Gendimenico GJ, et al. A pleiotropic response is induced in F9 embryonal carcinoma cells and rhino mouse skin by All-trans-retinoic acid, a RAR agonist but not by SR11237, a RXR-selective agonist. J Invest Dermatol. 1994;102(5):676-680.

[2]. Dupuis H, et al. Exposure to the RXR Agonist SR11237 in Early Life Causes Disturbed Skeletal Morphogenesis in a Rat Model. Int J Mol Sci. 2019;20(20):5198. Published 2019 Oct 20.

[3]. H.L. Dupuis. The RXR agonist SR-11237 affects skeletal development. ABSTRACT ONLY| VOLUME 24, SUPPLEMENT 1, S147, APRIL 01, 2016.

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Atazanavir(Synonyms: 阿扎那韦; BMS-232632)

发表于2024年2月12日由上海金畔生物科技有限公司

Atazanavir (Synonyms: 阿扎那韦; BMS-232632)

Atazanavir (BMS-232632) 是一种高选择性的 HIV-1蛋白酶抑制剂，用于艾滋病毒感染的研究。Atazanavir 是 CYP3A4 的底物和抑制剂，也是 P-糖蛋白的抑制剂和诱导剂。Atazanavir 也是 SARS-CoV 3CL^pro 的抑制剂，IC₅₀ 为 3.49 μM。

Atazanavir Chemical Structure

CAS No. : 198904-31-3

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

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Atazanavir 的其他形式现货产品:

Atazanavir sulfate

生物活性

Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration^[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)^[2]. Atazanavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 3.49 μM^[3].

IC₅₀ & Target

HIV-1 protease^[1]
CYP3A4, P-gp^[2]

Clinical Trial

分子量

704.86

Formula

C₃₈H₅₂N₆O₇

CAS 号

198904-31-3

中文名称

阿扎那韦

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]. Havlir DV, et al. Atazanavir: new option for treatment of HIV infection. Clin Infect Dis. 2004 Jun 1;38(11):1599-604.

[2]. Wood R. Atazanavir: its role in HIV treatment. Expert Rev Anti Infect Ther. 2008 Dec;6(6):785-96.

[3]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.

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BMS-8

发表于2023年12月29日由上海金畔生物科技有限公司

BMS-8

BMS-8 抑制 PD-1/PD-L1 相互作用，其 IC₅₀ 值为 7.2 μM。BMS-8 直接与 PD-L1 结合，可诱导 PD-L1 同源二聚体的形成，从而阻止其与 PD-1 的相互作用。

BMS-8 Chemical Structure

CAS No. : 1675201-90-7

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	BMS-8 inhibits the PD-1/PD-L1 interaction with IC₅₀ of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1^[1].
体外研究 (In Vitro)	BMS-8 tends to have a more stable binding mode with one PD-L1 monomer than the other and the small-molecule inducing PD-L1 dimerization was further stabilized by the non-polar interaction of Ile54, Tyr56, Met115, Ala121, and Tyr123 on both monomers and the water bridges involved in ALys124^[2]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	494.42
Formula	C₂₇H₂₈BrNO₃
CAS 号	1675201-90-7
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]. Eun-Hye Kim, et al. Preparation of Biphenyl-Conjugated Bromotyrosine for Inhibition of PD-1/PD-L1 Immune Checkpoint Interactions. Int J Mol Sci. 2020 May 21;21(10):3639. [2]. Danfeng Shi, et al. Computational Insight Into the Small Molecule Intervening PD-L1 Dimerization and the Potential Structure-Activity Relationship. Front Chem. 2019 Nov 12;7:764.

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BMS-8

发表于2023年12月28日由上海金畔生物科技有限公司

BMS-8

BMS-8 抑制 PD-1/PD-L1 相互作用，其 IC₅₀ 值为 7.2 μM。BMS-8 直接与 PD-L1 结合，可诱导 PD-L1 同源二聚体的形成，从而阻止其与 PD-1 的相互作用。

BMS-8 Chemical Structure

CAS No. : 1675201-90-7

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	BMS-8 inhibits the PD-1/PD-L1 interaction with IC₅₀ of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1^[1].
体外研究 (In Vitro)	BMS-8 tends to have a more stable binding mode with one PD-L1 monomer than the other and the small-molecule inducing PD-L1 dimerization was further stabilized by the non-polar interaction of Ile54, Tyr56, Met115, Ala121, and Tyr123 on both monomers and the water bridges involved in ALys124^[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	494.42
Formula	C₂₇H₂₈BrNO₃
CAS 号	1675201-90-7
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]. Eun-Hye Kim, et al. Preparation of Biphenyl-Conjugated Bromotyrosine for Inhibition of PD-1/PD-L1 Immune Checkpoint Interactions. Int J Mol Sci. 2020 May 21;21(10):3639. [2]. Danfeng Shi, et al. Computational Insight Into the Small Molecule Intervening PD-L1 Dimerization and the Potential Structure-Activity Relationship. Front Chem. 2019 Nov 12;7:764.

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BMS-8

发表于2023年12月28日由上海金畔生物科技有限公司

BMS-8

BMS-8 抑制 PD-1/PD-L1 相互作用，其 IC₅₀ 值为 7.2 μM。BMS-8 直接与 PD-L1 结合，可诱导 PD-L1 同源二聚体的形成，从而阻止其与 PD-1 的相互作用。

BMS-8 Chemical Structure

CAS No. : 1675201-90-7

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	BMS-8 inhibits the PD-1/PD-L1 interaction with IC₅₀ of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1^[1].
体外研究 (In Vitro)	BMS-8 tends to have a more stable binding mode with one PD-L1 monomer than the other and the small-molecule inducing PD-L1 dimerization was further stabilized by the non-polar interaction of Ile54, Tyr56, Met115, Ala121, and Tyr123 on both monomers and the water bridges involved in ALys124^[2]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	494.42
Formula	C₂₇H₂₈BrNO₃
CAS 号	1675201-90-7
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]. Eun-Hye Kim, et al. Preparation of Biphenyl-Conjugated Bromotyrosine for Inhibition of PD-1/PD-L1 Immune Checkpoint Interactions. Int J Mol Sci. 2020 May 21;21(10):3639. [2]. Danfeng Shi, et al. Computational Insight Into the Small Molecule Intervening PD-L1 Dimerization and the Potential Structure-Activity Relationship. Front Chem. 2019 Nov 12;7:764.

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BMS-195614(Synonyms: BMS 614)

发表于2023年12月22日由上海金畔生物科技有限公司

BMS-195614 (Synonyms: BMS 614)

BMS-195614 (BMS 614) 有效的中性视黄酸受体 RARα 选择性拮抗剂，K_i 值为 2.5 nM。

BMS-195614 Chemical Structure

CAS No. : 182135-66-6

规格		是否有货
100 mg		询价
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500 mg		询价

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生物活性	BMS-195614 (BMS 614) is a neutral RARα-selective antagonist with a K_i of 2.5 nM^[1].
分子量	448.51
Formula	C₂₉H₂₄N₂O₃
CAS 号	182135-66-6
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]. Géhin M, et al. Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists. Chem Biol. 1999;6(8):519-529.

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BMS-195614(Synonyms: BMS 614)

发表于2023年12月22日由上海金畔生物科技有限公司

BMS-195614 (Synonyms: BMS 614)

BMS-195614 (BMS 614) 有效的中性视黄酸受体 RARα 选择性拮抗剂，K_i 值为 2.5 nM。

BMS-195614 Chemical Structure

CAS No. : 182135-66-6

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	BMS-195614 (BMS 614) is a neutral RARα-selective antagonist with a K_i of 2.5 nM^[1].
分子量	448.51
Formula	C₂₉H₂₄N₂O₃
CAS 号	182135-66-6
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]. Géhin M, et al. Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists. Chem Biol. 1999;6(8):519-529.

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BMS-195614(Synonyms: BMS 614)

发表于2023年12月22日由上海金畔生物科技有限公司

BMS-195614 (Synonyms: BMS 614)

BMS-195614 (BMS 614) 有效的中性视黄酸受体 RARα 选择性拮抗剂，K_i 值为 2.5 nM。

BMS-195614 Chemical Structure

CAS No. : 182135-66-6

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	BMS-195614 (BMS 614) is a neutral RARα-selective antagonist with a K_i of 2.5 nM^[1].
分子量	448.51
Formula	C₂₉H₂₄N₂O₃
CAS 号	182135-66-6
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]. Géhin M, et al. Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists. Chem Biol. 1999;6(8):519-529.

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BMS641(Synonyms: BMS-209641)

发表于2023年11月29日由上海金畔生物科技有限公司

BMS641 (Synonyms: BMS-209641)

BMS641 (BMS-209641) 是一种选择性的 RARβ 激动剂。BMS641 对 RARβ (K_d，2.5 nM) 的亲和力比 RARα (K_d，225 nM) 或 RARγ (K_d, 223 nM) 的亲和力高100倍。

BMS641 Chemical Structure

CAS No. : 369364-50-1

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生物活性

BMS641 (BMS-209641) is a selective RARβ agonist. BMS641 has a higher affinity for RARβ (K_d, 2.5 nM) that is 100 times higher than that for RARα (K_d, 225 nM) or RARγ (K_d, 223 nM)^[1].

IC₅₀ & Target^[1]

RARβ

2.5 nM (Kd)

RARα

225 nM (Kd)

RARγ

223 nM (Kd)

分子量

414.92

Formula

C₂₇H₂₃ClO₂

CAS 号

369364-50-1

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]. Germain P, et al. Rational design of RAR-selective ligands revealed by RARbeta crystal stucture. EMBO Rep. 2004;5(9):877-882.

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BMS641(Synonyms: BMS-209641)

发表于2023年11月29日由上海金畔生物科技有限公司

BMS641 (Synonyms: BMS-209641)

BMS641 (BMS-209641) 是一种选择性的 RARβ 激动剂。BMS641 对 RARβ (K_d，2.5 nM) 的亲和力比 RARα (K_d，225 nM) 或 RARγ (K_d, 223 nM) 的亲和力高100倍。

BMS641 Chemical Structure

CAS No. : 369364-50-1

规格		是否有货
100 mg		询价
250 mg		询价
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生物活性

BMS641 (BMS-209641) is a selective RARβ agonist. BMS641 has a higher affinity for RARβ (K_d, 2.5 nM) that is 100 times higher than that for RARα (K_d, 225 nM) or RARγ (K_d, 223 nM)^[1].

IC₅₀ & Target^[1]

RARβ

2.5 nM (Kd)

RARα

225 nM (Kd)

RARγ

223 nM (Kd)

分子量

414.92

Formula

C₂₇H₂₃ClO₂

CAS 号

369364-50-1

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]. Germain P, et al. Rational design of RAR-selective ligands revealed by RARbeta crystal stucture. EMBO Rep. 2004;5(9):877-882.

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

BMS-986260

发表于2023年11月29日由上海金畔生物科技有限公司

BMS-986260

BMS-986260是一种免疫肿瘤学药物，是一种有效、选择性、口服活性的 TGFβR1 抑制剂 (IC₅₀=1.6 nM)。BMS-986260 对 TGFβR1 的选择性高于其同功酶 TGFβR2，并且在一组 200 多个被检测的激酶中也显示了这种选择性。BMS-986260 在 MINK 和 NHLF 细胞系中抑制 TGFβ 介导的 pSMAD2/3 核转位，IC₅₀ 分别为 350 nM 和 190 nM。

BMS-986260 Chemical Structure

CAS No. : 2001559-19-7

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

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生物活性	BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC₅₀=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC₅₀ of 350 nM and 190 nM, respectively^[1].
体外研究 (In Vitro)	BMS-986260 is a highly potent TGFβR1 inhibitor in both human (K_iapp=0.8 nM) and mouse (K_iapp= 1.4 nM) biochemical assays. BMS-986260 also inhibits TGFβ induced SMAD phosphorylation in NIH3T3 cell line, primary human T cells, and mouse and human whole blood. BMS-986260 inhibits TGF-β mediated induction of regulatory T cell (Treg) by downregulation of FOXP3 expression and a repression of CD25 with an IC₅₀ of 230 nM^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	382.78
Formula	C₁₈H₁₂ClFN₆O
CAS 号	2001559-19-7
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]. Velaparthi U, et al. Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent. ACS Med Chem Lett. 2020;11(2):172-178. Published 2020 Jan 28.

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

BMS641(Synonyms: BMS-209641)

发表于2023年11月29日由上海金畔生物科技有限公司

BMS641 (Synonyms: BMS-209641)

BMS641 (BMS-209641) 是一种选择性的 RARβ 激动剂。BMS641 对 RARβ (K_d，2.5 nM) 的亲和力比 RARα (K_d，225 nM) 或 RARγ (K_d, 223 nM) 的亲和力高100倍。

BMS641 Chemical Structure

CAS No. : 369364-50-1

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

BMS641 (BMS-209641) is a selective RARβ agonist. BMS641 has a higher affinity for RARβ (K_d, 2.5 nM) that is 100 times higher than that for RARα (K_d, 225 nM) or RARγ (K_d, 223 nM)^[1].

IC₅₀ & Target^[1]

RARβ

2.5 nM (Kd)

RARα

225 nM (Kd)

RARγ

223 nM (Kd)

分子量

414.92

Formula

C₂₇H₂₃ClO₂

CAS 号

369364-50-1

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]. Germain P, et al. Rational design of RAR-selective ligands revealed by RARbeta crystal stucture. EMBO Rep. 2004;5(9):877-882.

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