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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Brivanib Alaninate (BMS-582664), 血管内皮生长因子受体抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Information
Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor againstVEGFR2withIC50of 25 nM.
In vitro
BMS-582664 inhibits VEGF-stimulated and FGF-stimulated proliferating of HUVECs with IC50 of 40 nM and 276 nM. BMS-582664 (2 μM) significantly inhibits VEGFR2, FGFR1, ERK1/2 and Akt phosphorylation in VEGF- and bFGF-stimulated SK-HEP1 cells and HepG-2 cells, while BMS-582664 alone has little effect on levels of phosphorylated ERK1/2, Akt, VEGFR2, and FGFR1 in nonstimulated cells. BMS-582664 inhibits CYP2C19, CYP3A4(BFC) and CYP3A4 (BzRes) with IC50 of 2.4 μM, 0.51 μM and 1.6 μM, respectively. BMS-582664 exhibits high solid state stability (only 0.3% degradation at 50℃ with desiccant over a period of 12 weeks) and acceptable solution state stability up to pH 6.5.
In vivo
BMS-582664 (50 mg/kg) results in AUC of 136 μM×hr and Cmax of 41 μM in mouse. BMS-582664 (60 mg/kg, orally) is rapidly absorbed with Tmax of 1 hour, a favorable half-life (t1/2) of 2.7 hours and mean residence time (MRT) of 3.6 hours in mouse. BMS-582664 (25 mg/kg) results in AUC of 13.4 μM×hr and Cmax of 6.4 μM in rat. BMS-582664 dose-dependently inhibits the growth of established tumors with tumor growth inhibition of 85% and 97% at dose of 60 mg/kg and 90 mg/kg in H3396 xenografts athymic mice. BMS-582664 inhibits the growth rate of tumors in mice with patient-derived xenograft line 06-0606 by 55% and 13% at dose of 50 mg/kg and 100 mg/kg. BMS-582664 (60 mg/kg, orally) significantly reduces tumor weight at sacrifice, increases apoptosis, reduces microvessel density, inhibits of cell proliferation, and down-regulates cell cycle regulators in mice with patient-derived xenograft line 06-0606. BMS-582664 dose-dependently inhibits the growth of established tumors with tumor growth inhibition of 85% and 97% at dose of 80 mg/kg and 107 mg/kg in a L2987 nonsmall cell lung tumor xenografts assay in athymic mice. BMS-582664 (100 mg/kg) significantly modulates tyrosine kinase receptor 1 (Tie-1), collagen type IV alpha1 (Col4a1), complement component 1, q subcomponent receptor 1 (C1qr1), angiotensin receptor-like 1 (Agtrl1), and vascular endothelial-cadherin (Cdh5) in L2987 nonsmall cell lung tumor xenografts assay in athymic mice. BMS-582664 (100 mg/kg) inhibits the new growth of endothelial cells in two xenografts mouse models, L2987 and HCT116.
Cell Data
cell lines：HUVEC, HUASMC, and BRP cell lines
Concentrations：276 nM
Incubation Time：72 hours
Powder Purity:≥97%
规格
别名
布立尼布丙氨酸盐 (BMS-582664)
英文别名
(S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-yl) 2-aminopropanoate
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Brivanib Alaninate (BMS-582664)
生化机理
Brivanib alaninate（BMS-582664）是 BMS-540215 的原药，BMS-540215 是一种 ATP 竞争性 VEGFR2 抑制剂，IC50 为 25 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
血管内皮生长因子受体抑制剂
名称和识别符
EC号
639-686-7
分子类型
小分子
Isomeric SMILES
CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NN4C3=C(C(=C4)OC[C@@H](C)OC(=O)[C@H](C)N)C
分子量
441.46
Reaxy-Rn
36169984
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=36169984&ln=
技术文档
高级数据
产品属性
| ALogP | 3.1 |
|---|
关联靶点（人）
NUAK2
Tchem
NUAK 家族 SNF1 类激酶 2(NUAK family SNF1-like kinase 2)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 3 mg/mL (12.13 mM); Water: Insoluble; Ethanol: Insoluble;
安全和危险性（GHS）
信号词
Danger
危险声明
H373: 通过长时间或反复暴露对器官造成损害
H302: 吞食有害
H360: 可能损害生育力或未出生的孩子
H361: 怀疑破坏生育力或未出生的孩子
预防措施声明
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P405: 密闭存放
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P203: 使用前，获取、阅读并遵守所有安全说明。
P301+P317: 如果被吞咽：请寻求医疗帮助。
P318: 如果暴露或担心，请就医。
P319: 如果你感到不适，请寻求医疗帮助。
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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