873837-23-1|BMS-599626 Hydrochloride|BMS-599626 Hydrochloride|-范德生物科技公司

BMS-599626 Hydrochloride

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names：
BMS-599626 Hydrochloride
CAS号：
873837-23-1
MDL Number：
MF(分子式)： C27H28ClFN8O3 MW(分子量)： 567.01
EINECS: Reaxys Number:
Pubchem ID: Brand:

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询价

中文别名	BMS-599626 Hydrochloride(cas:873837-23-1)
英文别名	BMS-599626 Hydrochloride,873837-23-1
CAS号	873837-23-1
SMILES	O=C(OC[C@H]1NCCOC1)NC2=CN(C3=C2C)N=CN=C3NC4=CC5=C(C=C4)N(CC6=CC(F)=CC=C6)N=C5.Cl
Inchi
InchiKey
分子式 Formula	C27H28ClFN8O3
分子量 Molecular Weight	567.01
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility	生物体外In Vitro:DMSO溶解度100 mg/mL(176.36 mM;Need ultrasonic)
性状	固体粉末,Power
储藏条件 Storage conditions	-20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

BMS-599626 Hydrochloride(CAS:873837-23-1)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

产品说明	(CAS:873837-23-1)BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. IC50 value: 20 nM (HER1); 30 nM (HER2)
Introduction	BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. IC50 value: 20 nM (HER1); 30 nM (HER2) [1] Target: HER1/HER2 in vitro: BMS-599626 inhibited HER1 and HER2 with IC50 of 20 and 30 nmol/L, respectively, and was highly selective when tested against a broad panel of diverse protein kinases. Biochemical studies suggested that BMS-599626 inhibited HER1 and HER2 through distinct mechanisms. BMS-599626 abrogated HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50 in the range of 0.24 to 1 micromol/L. BMS-599626 was highly selective for tumor cells that depend on HER1/HER2 and had no effect on the proliferation of cell lines that do not express these receptors. In tumor cells that are capable of forming HER1/HER2 heterodimers, BMS-599626 inhibited heterodimerization and downstream signaling [1]. At the molecular level, in HN-5 cells the agent inhibited the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. The drug also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of γ-H AX foci up to 24 h after radiation [2]. in vivo: BMS-599626 had antitumor activity in models that overexpress HER1 (GEO), as well as in models that have HER2 gene amplification (KPL4) or overexpression (Sal2), and there was good correlation between the inhibition of receptor signaling and antitumor activity [1]. The drug given before and during irradiation improved the radioresponse of HN5 tumors in vivo [2].
Application1
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警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

【1】.Wong TW, 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 Oct 15;12(20 Pt 1):6186-93.

【2】.Torres MA, et al. AC480, formerly BMS-599626, a pan Her inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in vivo. Invest New Drugs. 2011 Aug;29(4):554-61.

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