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曲美替尼 (GSK1120212)

规格或纯度: ≥98%
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T127461-10mg 10mg 现货 Stock Image
T127461-50mg 50mg 现货 Stock Image
T127461-100mg 100mg 现货 Stock Image
T127461-250mg 250mg 现货 Stock Image
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mitogen-activated protein kinase kinase 1 Inhibitor mitogen-activated protein kinase kinase 2 Inhibitor
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基本描述

规格或纯度 ≥98%
英文名称 Trametinib (GSK1120212)
别名 曲美替尼; JTP 74057; GSK1120212
英文别名 GSK-1120212; JTP 74057; GSK1120212; GSK 1120212; JTP-74057; JTP74057;N-[3-[3-Cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]acetamide
生化机理 Trametinib is an allosteric reversible, selective MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2.
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 500mg卖完停产，不再备货
产品介绍

Trametinib (GSK1120212)是一种高特异性的，有效的MEK1/2抑制剂，IC50为0.92 nM/1.8 nM，对c-Raf， B-Raf， ERK1/2没有抑制活性。An allosteric inhibitor of MEK1/MEK2.

Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2.
An allosteric inhibitor of MEK1/MEK2.

名称和标识符

IUPAC Name N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide
INCHI InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34)
InChi Key LIRYPHYGHXZJBZ-UHFFFAOYSA-N
Canonical SMILES CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC=CC(=C4)NC(=O)C)C5CC5
分子式

C26H23FIN5O4
PubChem CID 11707110
分子量 615.39

化学和物理性质

溶解性 Soluble in DMSO (100 mg/mL at 25 °C), water (<1 mg/mL at 25 °C), ethanol (<1 mg/mL at 25 °C), and 30% PEG400/0.5% Tween80/5% propylene glycol (15 mg/ml).

安全信息

象形图
ghs08

Health Hazard

ghs07

Harmful
信号词 Danger
危险声明 H317: May cause an allergic skin reaction
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 P261,P280,P302+P352,P321,P405,P501,P264,P260,P270,P272,P333+P313,P362+P364,P203,P318,P319

靶标

Target ID 2062
名称 mitogen-activated protein kinase kinase 1
缩写名 MEK1
家族 STE7 family
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 393 15q22.31 MAP2K1 mitogen-activated protein kinase kinase 1
Mouse 2 393 9 34.55 cM Map2k1 mitogen-activated protein kinase kinase 1
Rat 2 393 8q24 Map2k1 mitogen activated protein kinase kinase 1
Ensembl Gene ENSG00000169032 (Hs) , ENSMUSG00000004936 (Mm) , ENSRNOG00000010176 (Rn)
Entrez Gene 5604 (Hs) , 26395 (Mm) , 170851 (Rn)
OMIM 176872 (Hs)
UniProtKB P31938 (Mm) , Q01986 (Rn) , Q02750 (Hs)
RefSeq Nucleotide NM_002755 (Hs) , NM_008927 (Mm) , NM_031643 (Rn)
RefSeq Protein NP_002746 (Hs) , NP_032953 (Mm) , NP_113831 (Rn)
Orphanet 123135 (Hs)
Protein GI 5579478 (Hs) , 6678794 (Mm) , 13928886 (Rn)
DrugBank Target Q02750 (Hs)
ChEMBL Target CHEMBL3587 (Hs) , CHEMBL5860 (Mm)
Target ID 2063
名称 mitogen-activated protein kinase kinase 2
缩写名 MEK2
家族 STE7 family
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 400 19p13.3 MAP2K2 mitogen-activated protein kinase kinase 2
Mouse 2 401 10 39.72 cM Map2k2 mitogen-activated protein kinase kinase 2
Rat 2 400 7q11 Map2k2 mitogen activated protein kinase kinase 2
Ensembl Gene ENSG00000126934 (Hs) , ENSMUSG00000035027 (Mm) , ENSRNOG00000020005 (Rn)
Entrez Gene 5605 (Hs) , 26396 (Mm) , 58960 (Rn)
OMIM 601263 (Hs)
UniProtKB P36506 (Rn) , P36507 (Hs) , Q63932 (Mm)
RefSeq Nucleotide NM_023138 (Mm) , NM_030662 (Hs) , NM_133283 (Rn)
RefSeq Protein NP_075627 (Mm) , NP_109587 (Hs) , NP_579817 (Rn)
Orphanet 123140 (Hs)
Protein GI 13489054 (Hs) , 31560267 (Mm) , 18959214 (Rn)
DrugBank Target P36507 (Hs)
ChEMBL Target CHEMBL2964 (Hs)

关联配体

Ligand ID 6495
名称 trametinib
别名 Mekinist®
类别 Synthetic organic
学名 N-[3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxopyrido[3,4-e]pyrimidin-1-yl]phenyl]acetamide
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 Trametinib is a Type-3 kinase inhibitor. Marketed formulations contain trametinib dimethyl sulfoxide (PubChem CID 50992434).

参考文献

1. Gilmartin AG, Bleam MR, Groy A, Moss KG, Minthorn EA, Kulkarni SG, Rominger CM, Erskine S, Fisher KE, Yang J et al..  (2011)  GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition..  Clin Cancer Res,  17  (5):  (989-1000).  [PMID:21245089]

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