产品名称

英文名称：Dabrafenib

同义词

GSK-2118436A、GSK-2118436、AKOS024463285、CCG-264736、N-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide、P06、Q413328、Dabrafenib (Free Base)、DB08912、DABRAFENIB [MI]、GSK2118436A、BRD-K09951645-0、达拉菲尼

产品性质

CAS编号：1195765-45-7

分子式：C23H20F3N5O2S2

分子量：519.56

PubChem编号：44462760

别名：达拉菲尼

英文别名：GSK-2118436A|GSK-2118436|AKOS024463285|CCG-264736|N-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide|P06|Q413328|Dabrafenib (Free Base)|DB08912|DABRAFENIB [MI]|GSK2118436A|BRD-K09951645-0

规格或纯度：≥98%

英文名称：Dabrafenib

生化机理：Dabrafenib is an orally bioavailable inhibitor of B-raf (BRAF) protein with potential antineoplastic activity. Dabrafenib selectively binds to and inhibits the activity of B-raf, which may inhibit the proliferation of tumor cells which contain a mutated BRAF gene. B-raf belongs to the the raf/mil family of serine/threonine protein kinases and plays a role in regulating the MAP kinase/ERKs signaling pathway, which may be constitutively activated due to BRAF gene mutations.Potent, ATP-competitive mutant B-Raf V600E inhibitor\xa0(IC 50 = 0.7 nM), with selectivity versus wild-type B-Raf (IC 50 =\xa05.2 nM) and c-RAf (IC 50 =\xa06.3 nM) in cell-free assays.\xa0Antitumor activity in vivo in mouse models of B-Raf V600E melanoma.

储存温度：-20°C储存

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：Dabrafenib (达拉菲尼; GSK2118436)是高活性BRAFV600特异性抑制剂，IC50为0.8 nM，比对野生型B-Raf和c-Raf的抑制性高4倍和6倍。A potent and selective inhibitor of Raf-B protein kinase carrying V600E mutationDabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM in cell-free assays, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively.A potent and selective inhibitor of Raf-B protein kinase carrying V600E mutation

IUPAC Name：N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide

INCHI：InChI=1S/C23H20F3N5O2S2/c1-23(2,3)21-30-18(19(34-21)16-10-11-28-22(27)29-16)12-6-4-9-15(17(12)26)31-35(32,33)20-13(24)7-5-8-14(20)25/h4-11,31H,1-3H3,(H2,27,28,29)

InChi Key：BFSMGDJOXZAERB-UHFFFAOYSA-N

Canonical SMILES：CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F

Isomeric SMILES：CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F

PubChem CID：44462760

ChEMBL Ligand：CHEMBL2028663

CAS Registry No.：1195765-45-7

Wikipedia：Dabrafenib

DrugBank Ligand：DB08912

RCSB PDB Ligand：P06

PEP：dabrafenib

Reactome Reaction：R-HSA-6802938

Reactome Drug：R-ALL-6802252

DrugCentral Ligand：4801

溶解性：DMSO 30 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

密度：1.4

折光率：1.63

沸点：~653.7 °C at 760 mmHg

象形图：

信号词：Warning

危险声明：H373 Causes damage to organs through prolonged or repeated exposureH411 Toxic to aquatic life with long lasting effectsH400 Very toxic to aquatic lifeH361 Suspected of damaging fertility or the unborn child

预防措施声明：P273,P280,P405,P501,P260,P391,P203,P318,P319

产品包装