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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
---|---|---|---|---|
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 | |
别名 | 达沙替尼; BMS 354825 |
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英文别名 | BMS-354825;Sprycel;BMS354825;BMS 354825; N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide |
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. |
EC号 | 801-607-0 |
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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 |
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 |
CAS Registry No. | 302962-49-8 |
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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 |
溶解性 | Soluble in DMSO (200 mg/mL), ethanol (very poorly ), and water (very poorly ). |
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敏感性 | 对空气和热敏感 |
象形图 |
Toxic Health Hazard Environmental Hazard Corrosive Harmful |
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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 |
输入批号以搜索COA:
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] |