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Mutant IDH1 inhibitor Sale

(Synonyms: (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) 目录号 : GC36665

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 Chemical Structure

Cas No.:1429180-08-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,034.00
现货
2mg
¥1,321.00
现货
5mg
¥1,845.00
现货
10mg
¥3,150.00
现货
50mg
¥9,450.00
现货
100mg
¥11,889.00
现货
200mg 待询 待询
500mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

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

产品描述

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

Chemical Properties

Cas No. 1429180-08-4 SDF
别名 (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
Canonical 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
溶解度 DMSO: ≥ 34 mg/mL (72.87 mM) 储存条件 Store at -20°C
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溶解性数据

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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
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Research Update

A Brain Penetrant Mutant IDH1 inhibitor Provides In Vivo Survival Benefit

Sci Rep 2017 Oct 23;7(1):13853.PMID:29062039DOI:10.1038/s41598-017-14065-w.

Mutations in IDH1 are highly prevalent in human glioma. First line treatment is radiotherapy, which many patients often forego to avoid treatment-associated morbidities. The high prevalence of IDH1 mutations in glioma highlights the need for brain-penetrant IDH1 mutant-selective inhibitors as an alternative therapeutic option. Here, we have explored the utility of such an inhibitor in IDH1 mutant patient-derived models to assess the potential therapeutic benefits associated with intracranial 2-HG inhibition. Treatment of mutant IDH1 cell line models led to a decrease in intracellular 2-HG levels both in vitro and in vivo. Interestingly, inhibition of 2-HG production had no effect on in vitro IDH1 mutant glioma cell proliferation. In contrast, IDH1 mutant-selective inhibitors provided considerable survival benefit in vivo. However, even with near complete inhibition of intratumoral 2-HG production, not all mutant glioma models responded to treatment. The results suggest that disruption of 2-HG production with brain-penetrant inhibitors in IDH1 mutant gliomas may have substantial patient benefit.