sevenspikes.themes.common.filters
sevenspikes.themes.common.closemenu

BFH772,≥99% (HPLC)

别名:BFH-772;6-((6-(hydroxymethyl)pyrimidin-4-yl)oxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide

CAS:890128-81-1;分子式:C23H16F3N3O3;分子量: 439.39
制造商品牌: BSZH 科学公司
货号(SKU): B06243
CAS号: 890128-81-1
MDL号: MFCD30534392
增值税发票 √ 免费送货 √ 订货电话:010-68689484
¥15,598

产品描述

本品可溶于DMSO(87 mg/mL )和乙醇

General description

一种有效的可口服的VEGFR2抑制剂,IC50为3 nM。

The VEGF family including VEGF-A, VEGF-B, VEGF-C, VEGF-D, and PlGF signals through VEGFR1, VEGFR2, and VEGFR3 cell surface tyrosine kinase receptors that are located on the host vascular endothelium, lymphatic, and hematopoietic systems.
In vitro: BFH772 was highly effective at targeting VEGFR2 kinase, however, lost 500-fold potency on FLK-1, FLT-1, and FLT-4. BFH772 also targeted B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 inhibited the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases. BFH772 was selective against the kinases of EGFR, ERBB2, INS-R, and IGF-1R and against the cytoplasmic BCR-ABL kinase .
In vivo: The dose response curves of BFH772 at 0.3, 1, and 3 mg/kg showed that even at the lowest concentrations, this naphthalene-1-carboxamide inhibited VEGF induced tissue weight and TIE-2 levels but only reached statistical significance at 1 mg/kg and above. Moreover, BFH772 at 3 mg/kg orally dosed once per day could potently inhibit melanoma growth (54-90% for primary tumor and 71-96% for metastasis tumor) when compared with control ratios .

包括VEGF-A,VEGF-B,VEGF-C,VEGF-D和PlGF在内的VEGF家族通过位于宿主血管内皮,淋巴和造血系统上的VEGFR1,VEGFR2和VEGFR3细胞表面酪氨酸激酶受体发出信号。
体外:BFH772在靶向VEGFR2激酶方面非常有效,但是在FLK-1,FLT-1和FLT-4上丧失了500倍的效力。 BFH772还针对B-RAF,RET和TIE-2,尽管其效价至少低40倍。 BFH772抑制配体诱导的RET,PDGFR和KIT激酶的自磷酸化。 BFH772对EGFR,ERBB2,INS-R和IGF-1R激酶以及细胞质BCR-ABL激酶具有选择性。
体内:BFH772在0.3、1和3 mg / kg时的剂量反应曲线表明,即使在最低浓度下,萘-1-甲酰胺也能抑制VEGF诱导的组织重量和TIE-2水平,但仅在1毫克/千克及以上。此外,与对照组相比,每天口服3 mg / kg BFH772可以有效抑制黑色素瘤的生长(原发肿瘤为54-90%,转移肿瘤为71-96%)。

Properties

Iupac Name6-((6-(hydroxymethyl)pyrimidin-4-yl)oxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide
Inchi Code1S/C23H16F3N3O3/c24-23(25,26)15-4-2-5-16(10-15)29-22(31)20-6-1-3-14-9-18(7-8-19(14)20)32-21-11-17(12-30)27-13-28-21/h1-11,13,30H,12H2,(H,29,31)
Inchi KeyJNLSTLQFDDAULK-UHFFFAOYSA-N


安全信息

风险声明 (欧洲) 23/24/25
安全声明 (欧洲) 26-36
WGK德国 WGK 3
商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 99 | 欧洲Eur. ≥ 10 | 東京Tokyo ≥ 22 | 香港与北京 ≥ 32