产品名称

英文名称：Bosutinib (SKI-606)

同义词

SKI-606、WAY-173606、Bosutinib,SKI-606、BSPBio_001023、NCGC00241107-03、NSC799367、NSC-799367、4-(2,4-Dichloro-5-methoxy-phenylamino)-6-methoxy-7-[3-(4-methyl-piperazin-1-yl)propoxy]quinoline-3-carbonitrile、5018V4AEZ0、DB06616、SK 606、2-[4-(2,3-dihydro-1,4-benzodi、伯舒替尼

产品性质

CAS编号：380843-75-4

分子式：C26H29Cl2N5O3

分子量：530.45

PubChem编号：5328940

别名：伯舒替尼

英文别名：SKI-606|WAY-173606|Bosutinib,SKI-606|BSPBio_001023|NCGC00241107-03|NSC799367|NSC-799367|4-(2,4-Dichloro-5-methoxy-phenylamino)-6-methoxy-7-[3-(4-methyl-piperazin-1-yl)propoxy]quinoline-3-carbonitrile|5018V4AEZ0|DB06616|SK 606|2-[4-(2,3-dihydro-1,4-benzodi

规格或纯度：≥99%

英文名称：Bosutinib (SKI-606)

生化机理：Abl和Src激酶的双重抑制剂（在酶法测定中，Src的IC50 = 1.2 nM）。对慢性骨髓性白血病（CML）细胞显示抗增殖活性，并降低乳腺癌细胞系的运动性和侵袭性。在不依赖于锚定的Src转化的大鼠成纤维细胞（IC50 = 100 nM）中也表现出有效的抗增殖活性。与非Src家族激酶（例如生长因子受体酪氨酸激酶）相比，显示Src的选择性。

法律信息：Sold for research purposes under agreement from Pfizer Inc. - Not for human or veterinary use.

运输条件：常规运输

产品介绍：Bosutinib (SKI-606) is a potent c-Abl, Bcr-Abl, and Src-Abl kinase inhibitor, shown to effectively interfere with the progress of chronic myelogenous leukemia (CML). In a competitive study with Imatinib, Bosutinib was shown to inhibit Bcr-Abl kinase activity in CD34+ CML cells more potently than Imatinib. Activity of Src-Abl has been implicated in the development of other non-CML malignancies, and Bosutinib has demonstrated in studies to suppress breast cancer growth and migration.A c-Abl, Src-Abl, and Bcr-Abl inhibitorBosutinib (SKI-606) is a potent c-Abl, Bcr-Abl, and Src-Abl kinase inhibitor, shown to effectively interfere with the progress of chronic myelogenous leukemia (CML). In a competitive study with Imatinib, Bosutinib was shown to inhibit Bcr-Abl kinase activity in CD34+ CML cells more potently than Imatinib. Activity of Src-Abl has been implicated in the development of other non-CML malignancies, and Bosutinib has demonstrated in studies to suppress breast cancer growth and migration.A c-Abl, Src-Abl, and Bcr-Abl inhibitor

ALogP：5.4

IUPAC Name：4-(2,4-dichloro-5-methoxyanilino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile

INCHI：InChI=1S/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-25-13-21-18(11-24(25)35-3)26(17(15-29)16-30-21)31-22-14-23(34-2)20(28)12-19(22)27/h11-14,16H,4-10H2,1-3H3,(H,30,31)

InChi Key：UBPYILGKFZZVDX-UHFFFAOYSA-N

Canonical SMILES：CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC

Isomeric SMILES：CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC

WGK Germany：3

PubChem CID：5328940

CAS Registry No.：380843-75-4

Wikipedia：Bosutinib

DiscoveRx TREEspot：SKI-606|

DrugBank Ligand：DB06616

ChEMBL Ligand：CHEMBL288441

RCSB PDB Ligand：DB8

PEP：bosutinib

DrugCentral Ligand：4359

溶解性：溶于DMSO, 最高浓度 (mg/mL) 53.05, 最高浓度(mM) 100；溶于ethanol, 最高浓度 (mg/mL) 13.26, 最高浓度(mM) 25

象形图：

危险声明：H315 Causes skin irritationH319 Causes serious eye irritationH335 May cause respiratory irritation

预防措施声明：P261,P305+P351+P338

产品包装