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阿西替尼

强效的VEGFR-1,-2和-3抑制剂
规格或纯度: ≥99%
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货号 (SKU) 包装规格 是否现货 价格 数量
A129732-10mg 10mg 现货 Stock Image
A129732-50mg 50mg 现货 Stock Image
A129732-250mg 250mg 现货 Stock Image
A129732-1g 1g 现货 Stock Image
A129732-5g 5g 期货 Stock Image

基本描述

规格或纯度 ≥99%
英文名称 Axitinib
别名 阿西替尼;N-甲基-2-((3-((1E)-2-(吡啶-2-基)乙烯)-1H-吲唑-6-基)硫)苯甲酰胺
英文别名 AG-013736; N-Methyl-2-((3-((1E)-2-(pyridin-2-yl)ethenyl)-1H-indazol-6-yl)sulfanyl)benzamide;Axitinib
生化机理 VEGFR-2,-3和-1的有效抑制剂(IC50值分别为0.2、0.1-0.3和1.2 nM)。对一组约100种蛋白激酶的活性最低。抑制血管生成和血管通透性。也是一种高亲和力的BCR-ABL1(T315I)抑制剂(自磷酸化ABL1(T315I)的Ki = 149 pM)。阻止表达BCR-ABL1(T315I)的Ba / F3细胞的增殖。口服。
应用 An inhibitor of Flt and Flk (VEGFR) with antitumor properties
法律信息 Sold for research purposes under agreement from Pfizer Inc. - Not for human or veterinary use.
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

Axitinib is a non-selective receptor kinase inhibitor of Flt and Flk proteins. This compound also inhibits Flt-1(VEGFR-1), Flk-1(VEGFR-2), Flt-4(VEGFR-3), PDGFR-β and c-Kit(c-KIT) with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively. Axitinib is studied as an antitumor agent of various cell lines. Axitinib is an inhibitor of PDGFR-β.An inhibitor of Flt and Flk (VEGFR) with antitumor properties

Axitinib is a non-selective receptor kinase inhibitor of Flt and Flk proteins. This compound also inhibits Flt-1(VEGFR-1), Flk-1(VEGFR-2), Flt-4(VEGFR-3), PDGFR-β and c-Kit(c-KIT) with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively. Axitinib is studied as an antitumor agent of various cell lines. Axitinib is an inhibitor of PDGFR-β.
An inhibitor of Flt and Flk (VEGFR) with antitumor properties

名称和标识符

IUPAC Name N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide
INCHI InChI=1S/C22H18N4OS/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14H,1H3,(H,23,27)(H,25,26)/b12-9+
InChi Key RITAVMQDGBJQJZ-FMIVXFBMSA-N
Canonical SMILES CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4
分子式

C22H18N4OS

PubChem CID 6450551
分子量 386.47

化学和物理性质

溶解性 溶于DMSO, 最高浓度 (mg/mL): 9.66, 最高浓度(mM): 25

安全信息

象形图
ghs08

Health Hazard

ghs09

Environmental Hazard

ghs07

Harmful

信号词 Warning
危险声明 H341: Suspected of causing genetic defects
H373: Causes damage to organs through prolonged or repeated exposure
H302: Harmful if swallowed
H400: Very toxic to aquatic life
H361: Suspected of damaging fertility or the unborn child
预防措施声明 P273,P280,P405,P501,P264,P260,P281,P270,P391,P330,P203,P301+P317,P318,P319
WGK Germany 3

靶标

Target ID 1813
名称 kinase insert domain receptor
缩写名 VEGFR-2
家族 Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family
别名 EBRT2
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 1356 4q12 KDR kinase insert domain receptor
Mouse 1 1367 5 40.23 cM Kdr kinase insert domain protein receptor
Rat 1 1343 14p11 Kdr kinase insert domain receptor
Ensembl Gene ENSG00000128052 (Hs) , ENSMUSG00000062960 (Mm) , ENSRNOG00000046829 (Rn)
Entrez Gene 16542 (Mm) , 25589 (Rn) , 3791 (Hs)
OMIM 191306 (Hs)
Protein GI 11321597 (Hs) , 27777648 (Mm) , 6981128 (Rn)
UniProtKB P35968 (Hs) , P35918 (Mm) , O08775 (Rn)
RefSeq Nucleotide NM_002253 (Hs) , NM_010612 (Mm) , NM_013062 (Rn)
RefSeq Protein NP_002244 (Hs) , NP_034742 (Mm) , NP_037194 (Rn)
Orphanet 229801 (Hs)
DrugBank Target P35968 (Hs)
CATH/Gene3D 2.60.40.10 (N/A)
ChEMBL Target CHEMBL3337 (Mm) , CHEMBL279 (Hs)
Target ID 2171
名称 polo like kinase 4
缩写名 PLK4
家族 Polo-like kinase (PLK) family
别名 Gpr41
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 970 4q28.1 PLK4 polo like kinase 4
Mouse 2 925 3 B Plk4 polo like kinase 4
Rat 2 924 2q25 Plk4 polo-like kinase 4
Ensembl Gene ENSG00000142731 (Hs) , ENSMUSG00000025758 (Mm) , ENSRNOG00000011654 (Rn)
Entrez Gene 10733 (Hs) , 20873 (Mm) , 310344 (Rn)
OMIM 605031 (Hs)
UniProtKB B2GUY1 (Rn) , O00444 (Hs) , Q64702 (Mm)
RefSeq Nucleotide NM_001107669 (Rn) , NM_001190799 (Hs) , NM_011495 (Mm)
RefSeq Protein NP_001101139 (Rn) , NP_055079 (Hs) , NP_775261 (Mm)
Protein GI 121114283 (Hs) , 358438436 (Mm) , 157818171 (Rn)
CATH/Gene3D 3.30.1120.30 (N/A)
ChEMBL Target CHEMBL3788 (Hs)

关联配体

Ligand ID 5659
名称 axitinib
别名 AG013736
类别 Synthetic organic
学名 N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-1H-indazol-6-yl}sulfanyl)benzamide
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Axitinib is a Type-1 kinase inhibitor. Axitinib inhibits several receptor tyrosine kinases including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and cKIT.

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