SGX-523

发表于由

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。

SGX-523  纯度: 99.28%

SGX523 是一种选择性和 ATP 竞争性的 MET 抑制剂。 SGX523 有效抑制 MET， IC50 为 4 nM ，比作用于其它他蛋白激酶的选择性高于 1,000 倍。具有抗肿瘤特性。

SGX-523

SGX-523 Chemical Structure

CAS No. : 1022150-57-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥870 In-stock
2 mg ￥660 In-stock
5 mg ￥1100 In-stock
10 mg ￥1600 In-stock
50 mg ￥5375 In-stock
100 mg ￥8500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SGX-523 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Orally Active Compound Library
  • Anti-Lung Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity[1].

体外研究
(In Vitro)

SGX523 shows ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD(0P), Ki=2.7 nM] versus the more active phospho-enzyme [MET-KD(3P), Ki=23 nM][1].
SGX523 inhibits the growth of gastric and lung cancer cell lines with amplification of the MET gene but has no effect, even at high micromolar concentration, on cell lines with normal MET gene copy number. TheIC50s of 0.02, 0.113, and 0.035 µM for NSCLC H1993, gastric cncer MKN45, and gastric cancer Hs746T cells, respectively[1].
The IC50 value for the inhibition of MET autophosphorylation is 0.040 μM in GTL16 cells[1].
SGX523 (0.5, 1.5, 4.6, 13.7, 41, 123, 370, 1100, 3300, 10000 nM; 1 hour) inhibits MET autophosphorylation without affecting total MET or extracellular signal-regulated kinase protein levels in HGF-stimulated A549 cells[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: Gastric cancer cell line GTL16
Concentration: 4.6, 14, 40, 120, 370, 1100, 3300, 10000 nM
Incubation Time: 1 hours
Result: Abolished constitutive signaling induced by MET gene amplification.

体内研究
(In Vivo)

SGX523 exhibits antitumor activity in vivo. SGX523 inhibits MET-dependent tumor growth[2].

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

Animal Model: Female Harlan nude mice (athymic nu/nu) were s.c. implanted with U87 cells[2]
Dosage: 10 or 30 mg/kg
Administration: Oral gavage; twice daily starting at day 5 for 22 days
Result: Potently inhibited U87MG tumor growth at a dose of 10 mg/kg administered twice daily.
Led to clear regression of U87MG tumors at 30 mg/kg dosed twice daily.

Clinical Trial

分子量

359.41

Formula

C18H13N7S
CAS 号

1022150-57-7
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 : 30 mg/mL (83.47 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7823 mL 13.9117 mL 27.8234 mL
5 mM 0.5565 mL 2.7823 mL 5.5647 mL
10 mM 0.2782 mL 1.3912 mL 2.7823 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:
  • 1.

    SGX-523 is prepared in 0.5% sodium carboxymethyl cellulose[2].
参考文献

  • [1]. Buchanan SG, et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther, 2009, 8(12), 3181-3190.

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