达沙替尼, Bcr/Abl 融合蛋白

强大的Src家族酪氨酸激酶（SFK）/ Bcl-Abl激酶抑制剂

规格或纯度: ≥99%

CAS编号: 302962-49-8
分子式: C₂₂H₂₆ClN₇O₂S
分子量: 488.01
EC号: 801-607-0
PubChem编号: 3062316

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货号 (SKU)	包装规格	是否现货
D125110-25mg	25mg	现货
D125110-100mg	100mg	现货
D125110-500mg	500mg	现货
D125110-1g	1g	现货
D125110-5g	5g	现货
D125110-25g	25g	现货

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基本描述

别名	达沙替尼
英文别名	BMS 354825\|AR-270/43507994\|Dasatinib (JAN/INN)\|HMS3744C11\|N-(2-CHLORO-6-METHYLPHENYL)-2-({6-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]-2-METHYLPYRIMIDIN-4-YL}AMINO)-1,3-THIAZOLE-5-CARBOXAMIDE\|SB17284\|Dasatinib - BMS-354825\|DTXSID50235486\|Pharmakon1600-01502275\|AB
规格或纯度	≥99%
英文名称	Dasatinib
生化机理	Dasatinib is more effective than imatinib in inhibiting the proliferation of Ba/F3 cells expressing wild-type Bcr-Abl and Bcr-Abl mutants, with the exception of T315I. Dasatinib has a two-log (～325-fold) increased potency relative to imatinib. Dasatinib is a potent wild-type and mutant c-Abl inhibitor, except T315I. Dasatinib directly targets wild-type and mutant c-Abl kinase domains and inhibits autophosphorylation and substrate phosphorylation in a concentration-dependent manner. Dasatinib displays 325-fold greater potency compared with imatinib against cells expressing wild-type Bcr-Abl. Dasatinib treatment inhibits SRC signaling, decreases growth, and induces cell cycle arrest and apoptosis in a subset of thyroid cancer cells.Potent Src family tyrosine kinase (SFK)/Bcl-Abl kinase inhibitor. Inhibits growth of Bcr-Abl–dependent chronic myeloid leukemia xenografts in nude mice. Anti-tumor activity in vivo .
储存温度	-20°C储存,充氩
运输条件	超低温冰袋运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？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	Dasatinib是一种Src/Abl抑制剂，对生型Abl和Src激酶均有抑制作用，IC50分别为0.6 nM和0.8 nM。Directly targets wild-type and mutant c-Abl kinase domains Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively. Directly targets wild-type and mutant c-Abl kinase domains

ALogP	3.6

名称和标识符

EC号	801-607-0
IUPAC Name	N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide
INCHI	InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
InChi Key	ZBNZXTGUTAYRHI-UHFFFAOYSA-N
Canonical SMILES	CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO
Isomeric SMILES	CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO
关联CAS	302962-49-8,863127-77-9
PubChem CID	3062316
NSC Number	732517
MeSH Entry Terms	(18F)-N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide;354825, BMS;BMS 354825;BMS-354825;BMS354825;dasatinib;N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methyl
分子量	488.01

数据库链接

CAS Registry No.	302962-49-8
Wikipedia	Dasatinib
DrugBank Ligand	DB01254
DiscoveRx TREEspot	Dasatinib\|
PubChem CID	3062316
ChEMBL Ligand	CHEMBL1421
RCSB PDB Ligand	1N1
PEP	dasatinib
Reactome Reaction	R-HSA-9669855, R-HSA-9669854, R-HSA-9669900, R-HSA-9674430, R-HSA-9674095
Reactome Drug	R-ALL-9669723
DrugCentral Ligand	785

CAS Registry No.

302962-49-8

Wikipedia

Dasatinib

DrugBank Ligand

DB01254

DiscoveRx TREEspot

Dasatinib|

PubChem CID

3062316

ChEMBL Ligand

CHEMBL1421

RCSB PDB Ligand

1N1

PEP

dasatinib

Reactome Reaction

R-HSA-9669855, R-HSA-9669854, R-HSA-9669900, R-HSA-9674430, R-HSA-9674095

Reactome Drug

R-ALL-9669723

DrugCentral Ligand

785

化学和物理性质

溶解性	Soluble in DMSO (200 mg/mL), ethanol (very poorly ), and water (very poorly ).
敏感性	对空气和热敏感

安全和危险性（GHS）

象形图	Toxic Health Hazard Environmental Hazard Corrosive Harmful
信号词	Danger
危险声明	H315: Causes skin irritation H301: Toxic if swallowed H351: Suspected of causing cancer H318: Causes serious eye damage H410: Very toxic to aquatic life with long lasting effects H372: Causes damage to organs through prolonged or repeated exposure H361: Suspected of damaging fertility or the unborn child
预防措施声明	P273,P280,P302+P352,P321,P405,P501,P264,P260,P270,P362+P364,P391,P330,P203,P264+P265,P301+P316,P305+P354+P338,P318,P317,P332+P317,P319

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参考文献

1. O'Hare T, Walters DK, Stoffregen EP, Jia T, Manley PW, Mestan J, Cowan-Jacob SW, Lee FY, Heinrich MC, Deininger MW et al.. (2005) In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants.. Cancer Res, 65 (11): (4500-5). [PMID:15930265]
2. Ozanne J, Prescott AR, Clark K. (2015) The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases.. Biochem J, 465 (2): (271-9). [PMID:25351958]
3. Al-Asmakh M et al.. (2021) Dasatinib and PD-L1 inhibitors provoke toxicity and inhibit angiogenesis in the embryo.. Biomed Pharmacother, 134 (): (111134). [PMID:33341672]
4. Piepgras J et al.. (2022) Enhancement of Phosphorylation and Transport Activity of the Neuronal Glutamate Transporter Excitatory Amino Acid Transporter 3 by C3bot and a 26mer C3bot Peptide.. Front Cell Neurosci, 16 (): (860823). [PMID:35783090]
5. Tanaka Y et al.. (2022) Nectin cell adhesion molecule 4 regulates angiogenesis through Src signaling and serves as a novel therapeutic target in angiosarcoma.. Sci Rep, 12 (): (4031). [PMID:35256687]

达沙替尼, Bcr/Abl 融合蛋白

库存信息

库存信息

库存信息

库存信息

库存信息

库存信息

基本描述

产品属性

名称和标识符

数据库链接

化学和物理性质

安全和危险性（GHS）

质检证书(COA)

质检报告(COA)

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