产品名称

英文名称：Mubritinib (TAK 165)

同义词

TAK165、DNDI1268116、M3058、SCHEMBL50451、CCG-269433、Mubritinib (USAN/INN)、D04025、DTXSID501026014、[4-[4-[[2-[(E)-2-[4-(Trifluoromethyl)phenyl]ethenyl]-1,3-oxazol-4-yl]methoxy]phenyl]butyl]-1H-1,2,3-triazole、1-[4-[4-[[2-[(E)-2-[4-(Trifluoromethyl)phenyl]etheny、木利替尼

产品性质

CAS编号：366017-09-6

分子式：C25H23F3N4O2

分子量：468.47

MDL号：MFCD09954135

PubChem编号：6444692

别名：木利替尼

英文别名：TAK165|DNDI1268116|M3058|SCHEMBL50451|CCG-269433|Mubritinib (USAN/INN)|D04025|DTXSID501026014|[4-[4-[[2-[(E)-2-[4-(Trifluoromethyl)phenyl]ethenyl]-1,3-oxazol-4-yl]methoxy]phenyl]butyl]-1H-1,2,3-triazole|1-[4-[4-[[2-[(E)-2-[4-(Trifluoromethyl)phenyl]etheny

规格或纯度：≥99%

英文名称：Mubritinib (TAK 165)

生化机理：TAK 165 is a potent Neu (HER2) and Cdc2 p34 inhibitor with IC50 of 6 nM and 0.2μM, respectively. TAK 165 also inhibits Cdk2 (p33cdk2) and Cdk5 (p33cdk5). TAK 165 displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. TAK 165 exhibits potent antiproliferative effects in Neu-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth.Potent, highly selective, irreversible ErbB2 inhibitor (IC 50 = 6 nM). Shows potent antiproliferative effects (IC 50 = 5 nM, ErbB2 overexpressing cancer cell lines). Shows antitumor effects in vivo.

应用：A selective, potent, and irreversible ErbB2 and EGFR inhibitor.

储存温度：-20°C储存

运输条件：超低温冰袋运输

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产品介绍：Mubritinib (TAK 165)是一种有效的HER2/ErbB2抑制剂，IC50为6 nM；对EGFR， FGFR， PDGFR， JAK1， Src和Blk没有抑制活性。A selective, potent, and irreversible ErbB2 and EGFR inhibitor.Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk.A selective, potent, and irreversible ErbB2 and EGFR inhibitor.

ALogP：5.4

IUPAC Name：4-[[4-[4-(triazol-1-yl)butyl]phenoxy]methyl]-2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,3-oxazole

INCHI：InChI=1S/C25H23F3N4O2/c26-25(27,28)21-9-4-20(5-10-21)8-13-24-30-22(18-34-24)17-33-23-11-6-19(7-12-23)3-1-2-15-32-16-14-29-31-32/h4-14,16,18H,1-3,15,17H2/b13-8+

InChi Key：ZTFBIUXIQYRUNT-MDWZMJQESA-N

Canonical SMILES：C1=CC(=CC=C1CCCCN2C=CN=N2)OCC3=COC(=N3)C=CC4=CC=C(C=C4)C(F)(F)F

Isomeric SMILES：C1=CC(=CC=C1CCCCN2C=CN=N2)OCC3=COC(=N3)/C=C/C4=CC=C(C=C4)C(F)(F)F

PubChem CID：6444692

ChEMBL Ligand：CHEMBL1614707

CAS Registry No.：366017-09-6

Wikipedia：Mubritinib

溶解性：Soluble in DMSO (25 mg/mL) with warming; ethanol (1.7 mg/mL), and water (<1 mg/mL).

敏感性：对热敏感

熔点：154-166oC

产品包装