Mutant IDH1 inhibitor

目录号: GC36665纯度: >98.50%同义词: (4S)-3-[2-[[(1S)-1-[4-[(4-乙酰基-1-哌嗪基)甲基]苯基]乙基]氨基]-4-嘧啶基]-4-异丙基-2-恶唑烷酮
Mutant IDH1 inhibitor 是一个有效的突变型 IDH1 R132H 的抑制剂,IC50 值小于 72 nM。

Mutant IDH1 inhibitor
Cas No.: 1429180-08-4
规格价格库存数量操作
1mg¥612.00现货
1
5mg¥1,440.00现货
1
10mg¥2,520.00现货
1
10mM (in 1mL DMSO)¥1,478.00现货
1

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产品描述 Description

Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM. IC50: < 72 nM (mutant IDH1 R132H)

Mutant IDH1 inhibitor is a potent IDH1 R132H inhibitor, and used for the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer[1].

[1]. 3-Pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH and their preparation. Patent WO 2013046136 A1 20130404

实验参考方法 Experimental Reference Method

Cell experiment:

Day 1: cells are seeded in 384-well plates in triplicates for both the cell proliferation and 2HG assay, and incubated at 37°C, 95% Rh, 5% CO2 overnight. Day 2: compounds are serially diluted 1 :3 (10 point dilution from 10 mM solutions in DMSO) and delivered to the cell assay plates via acoustic dispenser, with final concentration ranging from 30 μM to 1.5 nM. The plates are returned to the incubator after treatment and incubated for 48 hours. Day 4 Proliferation assay: CTG is added to the assay plates and luminescence signal is read on the plate reader. Day 4 2HG assay : Extraction sample preparation consisted of aspirating all media from the assay plates, adding 70 μL of 90% methanol in water, dry ice incubation for 15 minutes, centrifuging at 2000 rpm for 30 min to ensure all particulates have settled, and transferring 30 μL of the supernatant into LC-MS ready plates. LC-MS analysis follows.

References:

[1]. 3-Pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH and their preparation. Patent WO 2013046136 A1 20130404

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号
1429180-08-4
同义词
(4S)-3-[2-[[(1S)-1-[4-[(4-乙酰基-1-哌嗪基)甲基]苯基]乙基]氨基]-4-嘧啶基]-4-异丙基-2-恶唑烷酮
SMILES
CC(C)[C@@H](COC1=O)N1C2=NC(N[C@@H](C)C3=CC=C(CN4CCN(C(C)=O)CC4)C=C3)=NC=C2
分子式
C25H34N6O3
分子量
466.58 g/mol
溶解性
DMSO: ≥ 34 mg/mL (72.87 mM)
保存条件
Store at -20&#176;C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol