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- 详细信息
- 询价记录
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
859853-30-8
- 规格：
10 mM * 1 mL/2 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1945.0 |
|---|---|---|---|
| 规格： | 2 mg | 产品价格： | ￥1600.0 |
| 规格： | 5 mg | 产品价格： | ￥1950.0 |
| 规格： | 10 mg | 产品价格： | ￥3100.0 |
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BMS-690514
CAS No. : 859853-30-8
MCE 国际站：BMS-690514
产品活性：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。
研究领域：JAK/STAT Signaling | Protein Tyrosine Kinase/RTK
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. 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.
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. 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.
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文献和实验Lacrimal Experimental Protocol (4/4/94)
/30/10% Percoll gradient and spin at 500 rpm for 15 min. 30. If doing antibody inhibition experiments, remove antibody and wash BMS two times with warm DMEM/gent (gel) or sterile PBS (coated wells). 31. Cells reside at 60/30% interface. Use
Immunostaining of Cells Adherent to Coverslips
, or in 6 well plates. Coat overnight (4°C) with 3 ml/dish or well of 40 µg/ml BMS made up in ddH2O. 2) Remove coating solution and block with 1% BSA for 4 hr at 4°C. 3) Isolate cells and plate at 6 x 105 cells/ml (3 ml/well). Allow cells to adhere for 1 hr
Immunostaining of Cells Adherent to Coverslips
. Coat overnight (4°C) with 3 ml/dish or well of 40 µg/ml BMS made up in ddH2O. 2) Remove coating solution and block with 1 BSA for 4 hr at 4°C. 3) Isolate cells and plate at 6 x 105
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