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JMV 449,Bcr-Abl/Lyn酪氨酸激酶的有效双重抑制剂, 酪氨酸蛋白激酶 Lyn 抑制剂

Bcr-Abl / Lyn酪氨酸激酶的有效和选择性双重抑制剂
规格或纯度: 95%
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货号 (SKU) 包装规格 是否现货 价格 数量
B129232-5mg
 5mg 现货 Stock Image
B129232-10mg
 10mg 现货 Stock Image
B129232-25mg
 25mg 现货 Stock Image
B129232-50mg
 50mg 现货 Stock Image
B129232-100mg
 100mg 现货 Stock Image
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基本描述

别名 巴非替尼
英文别名 NS-187|AS-13209|BAFETINIB [MART.]|Bafetinib [USAN:INN]|(S)-N-(3-(4,5'-bipyrimidin-2-ylamino)-4-methylphenyl)-4-((3-(dimethylamino)pyrrolidin-1-yl)methyl)-3-(trifluoromethyl)benzamide|GS-3022|NSC799354|NSC-799354|s1369|4-[[(3S)-3-(dimethylamino)pyrrolidin-
规格或纯度 95%
英文名称 Bafetinib (INNO-406)
生化机理 Bafetinib (1-10 μM) concentration dependently inhibits PAR2-TRPV4 coupling. In TRPV4 HEKs, 10 μM Bafetinib significantly inhibits the coupling response to SLIGRL and trypsin compared with vehicle control. Bafetinib inhibits the signalling pathway leading to TRPV4 channel opening, downstream of PAR2 activation, most likely by blocking the activation of a tyrosine kinase. Bafetinib blocks WT Bcr-Abl autophosphorylation and its downstream kinase activity with IC50 of 11 nM and 22 nM in K562 and 293T cells, respectively. Bafetinib suppresses the growth of the Bcr-Abl-positive cell lines including K562, KU812, and BaF3/wt cells potently without effects on the proliferation of the Bcr-Abl-negative U937 cell line. Moreover, Bafetinib exhibits a dose-dependent antiproliferative effect against Bcr-Abl point mutant cell lines, such as BaF3/E255K cells.Potent and selective orally bioavailable dual inhibitor of Bcr-Abl/Lyn tyrosine kinase with IC 50 values of 5.8nM and 19nM, respectively. Can block the autophosphorylation of Bcr-Abl. Highly potent to inhibit tumor growth in murine tumor models.
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 有关更多信息，请参阅SDS。有关溶解度，用法和处理的更多建议？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍

Bafetinib (INNO-406)是一种有效的，选择性的，Bcr-Abl/Lyn双重抑制剂，IC50为5.8 nM/19 nM，对T315I突变型的磷酸化没有抑制作用，对PDGFR和c-Kit的作用效果稍弱。

Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit.

产品属性

ALogP 4.2

名称和标识符

IUPAC Name 4-[[(3S)-3-(dimethylamino)pyrrolidin-1-yl]methyl]-N-[4-methyl-3-[(4-pyrimidin-5-ylpyrimidin-2-yl)amino]phenyl]-3-(trifluoromethyl)benzamide
INCHI InChI=1S/C30H31F3N8O/c1-19-4-7-23(13-27(19)39-29-36-10-8-26(38-29)22-14-34-18-35-15-22)37-28(42)20-5-6-21(25(12-20)30(31,32)33)16-41-11-9-24(17-41)40(2)3/h4-8,10,12-15,18,24H,9,11,16-17H2,1-3H3,(H,37,42)(H,36,38,39)/t24-/m0/s1
InChi Key ZGBAJMQHJDFTQJ-DEOSSOPVSA-N
Canonical SMILES CC1=C(C=C(C=C1)NC(=O)C2=CC(=C(C=C2)CN3CCC(C3)N(C)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CN=C5
Isomeric SMILES CC1=C(C=C(C=C1)NC(=O)C2=CC(=C(C=C2)CN3CC[C@@H](C3)N(C)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CN=C5
PubChem CID 11387605
分子量 576.62

化学和物理性质

溶解性 DMSO 115 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

安全和危险性（GHS）

象形图
ghs07

Harmful
信号词 Warning
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
预防措施声明 P261,P305+P351+P338

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参考文献

1. Horio T, Hamasaki T, Inoue T, Wakayama T, Itou S, Naito H, Asaki T, Hayase H, Niwa T.  (2007)  Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives..  Bioorg Med Chem Lett,  17  (10):  (2712-7).  [PMID:17376680]
2. Rix U, Remsing Rix LL, Terker AS, Fernbach NV, Hantschel O, Planyavsky M, Breitwieser FP, Herrmann H, Colinge J, Bennett KL et al..  (2010)  A comprehensive target selectivity survey of the BCR-ABL kinase inhibitor INNO-406 by kinase profiling and chemical proteomics in chronic myeloid leukemia cells..  Leukemia,  24  (1):  (44-50).  [PMID:19890374]
3. Niwa T, Asaki T, Kimura S.  (2007)  NS-187 (INNO-406), a Bcr-Abl/Lyn dual tyrosine kinase inhibitor..  Anal Chem Insights,  2  (13):  (93-106).  [PMID:19662183]
4. Kantarjian H, le Coutre P, Cortes J, Pinilla-Ibarz J, Nagler A, Hochhaus A, Kimura S, Ottmann O.  (2010)  Phase 1 study of INNO-406, a dual Abl/Lyn kinase inhibitor, in Philadelphia chromosome-positive leukemias after imatinib resistance or intolerance..  Cancer,  116  (11):  (2665-72).  [PMID:20310049]
5. Santos FP, Kantarjian H, Cortes J, Quintas-Cardama A.  (2010)  Bafetinib, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia..  Curr Opin Investig Drugs,  11  (12):  (1450-65).  [PMID:21154127]
6. Kimura S, Naito H, Segawa H, Kuroda J, Yuasa T, Sato K, Yokota A, Kamitsuji Y, Kawata E, Ashihara E et al..  (2005)  NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia..  Blood,  106  (12):  (3948-54).  [PMID:16105974]
7. Sterne GR et al..  (2015)  Dysregulated Dscam levels act through Abelson tyrosine kinase to enlarge presynaptic arbors..  Elife,  4  ():  ().  [PMID:25988807]
8. Yokota A et al..  (2007)  INNO-406, a novel BCR-ABL/Lyn dual tyrosine kinase inhibitor, suppresses the growth of Ph+ leukemia cells in the central nervous system, and cyclosporine A augments its in vivo activity..  Blood,  109  ():  (306-14).  [PMID:16954504]
9. Kamitsuji Y et al..  (2008)  The Bcr-Abl kinase inhibitor INNO-406 induces autophagy and different modes of cell death execution in Bcr-Abl-positive leukemias..  Cell Death Differ,  15  (11):  (1712-22).  [PMID:18617896]
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