Mutant IDH1 inhibitor

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Mutant IDH1 inhibitor  纯度: 98.69%

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

Mutant IDH1 inhibitor Chemical Structure

CAS No. : 1429180-08-4

规格 价格 是否有货 数量
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10 mM * 1 mL in DMSO ￥2260 In-stock
5 mg ￥2050 In-stock
10 mg ￥3500 In-stock
50 mg ￥10500 In-stock
100 mg ￥18000 In-stock
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500 mg   询价  

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生物活性

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

IC50 & Target

IC50: < 72 nM (mutant IDH1 R132H)
体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

466.58

Formula

C25H34N6O3
CAS 号

1429180-08-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 34 mg/mL (72.87 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1433 mL 10.7163 mL 21.4326 mL
5 mM 0.4287 mL 2.1433 mL 4.2865 mL
10 mM 0.2143 mL 1.0716 mL 2.1433 mL

*

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, 6 months; -20°C, 1 month。-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。
参考文献

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

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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

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

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