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BMS-599626 Hydrochloride Sale

(Synonyms: AC480;BMS-599626 HCl;BMS599626;BMS 599626;AC-480) 目录号 : GC10606

BMS-599626 Hydrochloride (AC480 Hydrochloride) 是一种选择性的口服生物可利用的 HER1 和 HER2 抑制剂,IC50 分别为 20 和 30 nM。 BMS-599626 Hydrochloride 对 HER4 (IC50=190 nM) 的效力降低约 8 倍,对 VEGFR2、c-Kit、Lck、MEK 的效力超过 100 倍。 BMS-599626 Hydrochloride 抑制肿瘤细胞增殖,并有可能增加肿瘤对放疗的反应。

BMS-599626 Hydrochloride Chemical Structure

Cas No.:873837-23-1

规格 价格 库存 购买数量
25mg 待询 待询
5mg
¥753.00
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100mg
¥6,278.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

BMS-599626 is a selective inhibitor of HER1 and HER2 with IC50 value of 22 nM and 32 nM, respectively [1].
HER (human epidermal growth factor receptor) is a member of EGFR/ErbB family and plays an important role in transduction of cell proliferation and differentiation. It has been reported that abbrent expression of HER is correlated with cancer and HER inhibition is being regarded as a promising strategy for cancer treatment [1].
BMS-599626 is a potent HER inhibitor and has the higher inhibition ability than the other reported inhibitors. When tested with breast tumor cell lines (HCC202, HCC1942 and AU565) that highly expressing HER1 and HER2, BMS-599626 treatment inhibited cell proliferation, while had no effect on A2780 cells that without HER1 or HER2 expression [1]. Treated OV202 cells with BMS-599626 significantly inhibited cell proliferation and enhanced cell apoptosis by inhibiting HER [2].
In mouse model with Sal2 tumor cells xenograft, oral administration of BMS-599626 inhibited Sal2 cells growth in a dose-dependent manner and significantly delayed tumor growth at the concentration of 60 mg/kg [1].
When tested with Sal2 cells expressing CD8-HER2 fusion protein, BMS-599626 treatment inhibited the receptor phosphorylation and MAPK phosphorylation with the IC50 value of 0.3 and 0.22 μM/L, respectively [1].
References:
[1].Wong, T.W., et al., Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res, 2006. 12(20 Pt 1): p. 6186-93.
[2].Haluska, P., et al., HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924. Mol Cancer Ther, 2008. 7(9): p. 2589-98.

Chemical Properties

Cas No. 873837-23-1 SDF
别名 AC480;BMS-599626 HCl;BMS599626;BMS 599626;AC-480
化学名 [(3S)-morpholin-3-yl]methyl N-[4-[[1-[(3-fluorophenyl)methyl]indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamate;hydrochloride
Canonical SMILES CC1=C2C(=NC=NN2C=C1NC(=O)OCC3COCCN3)NC4=CC5=C(C=C4)N(N=C5)CC6=CC(=CC=C6)F.Cl
分子式 C27H28ClFN8O3 分子量 567.01
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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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。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.7636 mL 8.8182 mL 17.6364 mL
5 mM 0.3527 mL 1.7636 mL 3.5273 mL
10 mM 0.1764 mL 0.8818 mL 1.7636 mL
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