CAS:871700-17-3Trametinib

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Trametinib N-[3-[3-环丙基-5-[(2-氟-4-碘苯基)氨基]-3,4,6,7-四氢-6,8-二甲基-2,4,7-三氧代吡啶并[4,3-d]嘧啶-1(2H)-基]苯基]乙酰胺 Cat No. FB03776Cas No. 871700-17-3

Synonyms: JTP-74057;GSK 1120212

Trametinib 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.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6250 mL
- 8.1248 mL
- 16.2496 mL
- 5 mM
- 0.3250 mL
- 1.6250 mL
- 3.2499 mL
- 10 mM
- 0.1625 mL
- 0.8125 mL
- 1.6250 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

871700-17-3

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C26H23FIN5O4

运输

蓝冰

分子量

615.39

别名

JTP-74057;GSK 1120212

溶解度

DMSO	100.0 mg/mL (162.5 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	2 mg/mL	clear
PO	0.5% CMC-Na	30 mg/mL	suspension

靶点数据

生物活性

靶点 MEK1

IC50:0.92nM MEK2

IC50:1.8nM
描述Trametinib, also called as GSK1120212 or JTP-74057, can strongly inhibit MEK1/2 kinase activities with IC50 value of 0.92nM and 1.8nM, respectively, without inhibition on the other 98 kinases (measured by Raf-MEK-ERK cascade kinase assay) regardless of the isotype of Raf and MEK. Trametinib can inhibit constitutive ERK phosphorylation (downstream of MEK) in cell lines, while the effect on anti-proliferation differs. Among them, HT-29 and COLO205 cells with a constitutively active B-Raf mutant were most sensitive to trametinib while COLO320 DM cells bearing the wild-type gene in both B-Raf and K-Ras were found to be resistant to trametinib. Oral treatment of trametinib 1mg/kg daily for 14 days blocked the tumor increase almost completely in nude mice bearing the HT-29 xenografts^[1].Trametinib is indicated for the treatment in patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations detected by an FDA-approved test^[2].
作用机制Trametinib binds to MEK1/2 and induces allosteric inhibition of MEK1/2 catalysis.^[3]
动物研究
剂量
Mice: min = 0.3 mg/kg^[1], max = 2 mg/kg^[2]

给药途径
p.o.

动物研究
剂量	Mice: min = 0.3 mg/kg^[1], max = 2 mg/kg^[2]
给药途径	p.o.

靶点	Description	IC50
MEK1		IC50:0.92nM
MEK2		IC50:1.8nM