Olutasidenib|1887014-12-1|(FT-2102)-陌孚医药/Medlife

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Olutasidenib (Synonyms: FT-2102)

目录号: PL02184 纯度: ≥99%

CAS No. :1887014-12-1

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中文名称	Olutasidenib
中文别名	Olutasidenib; FT-2102; FT 2102; FT210
英文名称	Olutasidenib
英文别名	5-[[(1S)-1-(6-Chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino]-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile;5-[1-(6-Chloro-2-oxo-1H-quinolin-3-yl)ethylamino]-1-methyl-6-oxopyridine-2-carbonitrile;Olutasidenib
Cas No.	1887014-12-1
分子式	C₁₈H₁₅ClN₄O₂
分子量	354.79
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Olutasidenib (FT-2102) 是一种，具有口服活性的、能透过血脑屏障的、突变型异柠檬酸脱氢酶 (IDH)1 的选择性有效抑制剂，对IDH1- R132H 和 IDH1- R132C的 IC₅₀ 值分别为 21.2 nM 和 114 nM。可用于研究急性髓性白血病或骨髓增生异常综合征。

生物活性

Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC 50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .

性状

Solid

IC50 & Target[1][2]

IC50: 21.2 nM (IDH1- R132H), 114 nM (IDH1- R132C).

体外研究(In Vitro)

Olutasidenib (FT-2102) potently inhibits 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), suggesting Olutasidenib (FT-2102) could be efficacious against most IDH1-R132 mutant-expressing tumors. Olutasidenib (FT-2102) is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 (> 20 μM) and IDH2 mutants (R172K and R140Q: both > 20 μM). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Olutasidenib (FT-2102, three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals) exhibits potent anti-tumor activity in HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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

ClinicalTrial

参考文献

[1]. JM Watts, et al. A phase 1 dose escalation study of the IDH1m inhibitor, FT-2102, in patients with acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS).
[2]. Justin A. Caravella, et al. Structure-based design and identification of FT-2102 (olutasidenib), a potent mutant-selective IDH1 inhibitor. J Med Chem. 2020.

溶解度数据	In Vitro: DMSO : 125 mg/mL (352.32 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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