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多维替尼 (TKI-258, CHIR-258)

强大的选择性III-V类受体酪氨酸激酶抑制剂
规格或纯度: ≥99%
有货

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库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
D126778-10mg
10mg 现货 Stock Image
D126778-50mg
50mg 现货 Stock Image
D126778-250mg
250mg 现货 Stock Image

基本描述

别名 多韦替尼
英文别名 CHIR-258|C75053|D77370|BDBM153731|GFKI-258|MFCD10565680|NCGC00249685-11|TK-258|AC-32059|B2693-091881|Dovitinib|Q27163255|SCHEMBL32934|1447274-99-8|4-AMINO-5-FLUORO-3-[ 5- (4-METHYLPIPERAZIN-1-YL)-1H-BENZIMIDAZOL-2-YL]QUINOLIN-2(1H)-ONE|TKI 258|UNII-I35H55
规格或纯度 ≥99%
英文名称 Dovitinib (TKI-258, CHIR-258)
生化机理 Dovitinib, Free Base, is the non-salt form of dovitinib, lactate salt (sc-396753). Dovitinib is a multitargeted growth factor receptor kinase inhibitor to VEGFR, FGFR3, PDGFR and c-KIT.Potent, selective inhibitor of class III-V receptor tyrosine kinases (RTKs). Inhibits FLT3 (IC 50 = 1 nM), c-KIT (IC 50 = 2 nM), FGFR (IC 50 = 8 nM), VEGFR1/2/3 (IC 50 values are\xa010 nM, 13 nM and 8 nM respectively)。
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

Dovitinib (TKI-258, CHIR-258)是一种多靶点的RTK抑制剂,对III型(FLT3/c-Kit)作用最强,IC50为1 nM/2 nM,同时也作用于IV类(FGFR1/3)和V类(VEGFR1-4) RTKs,IC50为8-13 nM,但对InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R和HER2作用较弱。The free base form of an FGFR inhibitor

Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2.
The free base form of an FGFR inhibitor

名称和标识符

IUPAC Name 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one
INCHI InChI=1S/C21H21FN6O/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29)
InChi Key PIQCTGMSNWUMAF-UHFFFAOYSA-N
Canonical SMILES CN1CCN(CC1)C2=CC3=C(C=C2)N=C(N3)C4=C(C5=C(C=CC=C5F)NC4=O)N
Isomeric SMILES CN1CCN(CC1)C2=CC3=C(C=C2)N=C(N3)C4=C(C5=C(C=CC=C5F)NC4=O)N
PubChem CID 135398510
分子量 392.43

化学和物理性质

溶解性 DMSO:34 mg/mL,Insoluble in water and Ethanol

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参考文献

1. Renhowe PA, Pecchi S, Shafer CM, Machajewski TD, Jazan EM, Taylor C, Antonios-McCrea W, McBride CM, Frazier K, Wiesmann M et al..  (2009)  Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors..  J Med Chem,  52  (2):  (278-92).  [PMID:19113866]