BMS-794833
目录号 : GC13833
An inhibitor of c-Met and VEGFR2
Cas No.:1174046-72-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
BMS-794833 is a potent ATP competitive, dual inhibitor of c-Met and VEGFR2 (IC50 = 1.7 nM and 15 nM, respectively). It also has inhibitory effect on Ron, Axl and Flt3 (IC50 < 3 nM).
c-MET, also called MET, is a membrane receptor that is essential for embryonic development and wound healing. VEGFR are receptors for vascular endothelial growth factor and belong to receptor tyrosine kinases. It mediates in various cellular functions, including endothelial proliferation, migration, survival, tubular morphogenesis and sprouting. [1]
BMS794833 also inhibited gastric cancer cell line (GTL-16) that induced by c-Met receptor, GTL-16, IC50 = 39 Nm [1]. In human gastric tumor xenografts model, BM798433 exhibits > 50% TGI for at least one tumor doubling time without significant toxicity in 14 days. In U87 glioblastoma model, 25mg/kg of BMS798433 exert complete tumor stasis. [1]
Reference:
[1] 4-pyridinone compounds and their use of cancer, Borzilleri et al, United States patent application publication, Pub No. : US 2012/0114643 A1, Pub.Date: May 10, 2012.
Cell experiment: | GTL-16 cells are inoculated in to 96 well microtiter plates in 0.5% fetal calf serum and incubated at 37°C, 5% CO2, 95% air and 100% relative humidity for 24 h prior to addition of a compound. Cells are treated with BMS-794833 for an additional 72 h. Growth inhibition is calculated[1]. |
References: [1]. WO2009094417 | |
| Cas No. | 1174046-72-0 | SDF | |
| 化学名 | N-[4-(2-amino-3-chloropyridin-4-yl)oxy-3-fluorophenyl]-5-(4-fluorophenyl)-4-oxo-1H-pyridine-3-carboxamide | ||
| Canonical SMILES | C1=CC(=CC=C1C2=CNC=C(C2=O)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F)F | ||
| 分子式 | C23H15ClF2N4O3 | 分子量 | 468.84 |
| 溶解度 | ≥ 23.45mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1329 mL | 10.6646 mL | 21.3292 mL |
| 5 mM | 0.4266 mL | 2.1329 mL | 4.2658 mL |
| 10 mM | 0.2133 mL | 1.0665 mL | 2.1329 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet