产品名称

英文名称：Linifanib (ABT-869)

同义词

Linifanib、796967-16-3、ABT-869、Linifanib (ABT-869)、1-(4-(3-amino-1H-indazol-4-yl)phenyl)-3-(2-fluoro-5-methylphenyl)urea、AL-39324、ABT 869、1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea、Linifanib (GMP)、N-[4-(3-amino-1H-indazol-4-yl)ph

产品性质

CAS编号：796967-16-3

分子式：C21H18FN5O

分子量：375.41

PubChem编号：11485656

英文别名：Linifanib|796967-16-3|ABT-869|Linifanib (ABT-869)|1-(4-(3-amino-1H-indazol-4-yl)phenyl)-3-(2-fluoro-5-methylphenyl)urea|AL-39324|ABT 869|1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea|Linifanib (GMP)|N-[4-(3-amino-1H-indazol-4-yl)ph

规格或纯度：≥99%

英文名称：Linifanib (ABT-869)

生化机理：ABT-869 is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (Flt/Flk) and PDGFR families (e.g., KDR, Flt1, Flt3, Flt4, CSF-1R, and KIT) demonstrating IC50 values ranging from 4-190 nM. ABT-869 shows little activity against unrelated RTKs, cytoplasmic tyrosine kinases, or Ser/Thr kinases (IC50 > 1 μM). ABT-869 inhibits proliferation in MV-4-11 and MOLM-13 cells (acute myeloid leukemia cell lines harboring RTK mutations; IC50 = 4 and 6 nM, respectively), inducing apoptosis as evidenced by an increased sub-G0/G1 phase cell population, caspase activation, and PARP cleavage. In murine xenograft models, as well as in a phase 1 clinical trial, ABT-869 demonstrated respectable efficacy in solid tumors including lung and hepatocellular carcinomas.

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：5mg、50mg卖完停产，不再备货

产品介绍：Linifanib (ABT-869)是一种新型，有效，ATP竞争性VEGFR/PDGFR抑制剂，同时抑制KDR， CSF-1R， Flt-1/3和PDGFRβ，其IC50分别为4 nM， 3 nM， 3 nM/4 nM和66 nM ，对具有突变激酶依赖性的癌细胞（即FLT3）最有效。Phase 3。A VEGF (Flk/Flt) and PDGFR inhibitor.Linifanib (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Phase 3.A VEGF (Flk/Flt) and PDGFR inhibitor.

ALogP：3.9

IUPAC Name：1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea

INCHI：InChI=1S/C21H18FN5O/c1-12-5-10-16(22)18(11-12)25-21(28)24-14-8-6-13(7-9-14)15-3-2-4-17-19(15)20(23)27-26-17/h2-11H,1H3,(H3,23,26,27)(H2,24,25,28)

InChi Key：MPVGZUGXCQEXTM-UHFFFAOYSA-N

Canonical SMILES：CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N

Isomeric SMILES：CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N

PubChem CID：11485656

CAS Registry No.：796967-16-3

Wikipedia：Linifanib

DiscoveRx TREEspot：ABT-869|

ChEMBL Ligand：CHEMBL223360

Reactome Reaction：R-HSA-9702508, R-HSA-9695828, R-HSA-9702997

Reactome Drug：R-ALL-9702979

溶解性：Soluble in water (<1 mg/ml) at 25 °C, DMSO (~20 mg/ml), DMF (~20 mg/ml), 15 DMSOPBS (pH 7.2) (~0.2 mg/ml), ethanol (5 mg/ml) at 25 °C, and methanol.

象形图：

信号词：Danger

危险声明：H400 Very toxic to aquatic lifeH410 Very toxic to aquatic life with long lasting effectsH372 Causes damage to organs through prolonged or repeated exposureH361 Suspected of damaging fertility or the unborn child

预防措施声明：P273,P280,P405,P501,P264,P260,P270,P391,P203,P318,P319

产品包装