Olutasidenib FT-2102|cas:1887014-12-1|西域试剂

Olutasidenib FT-2102,99.30%

产品编号：Bellancom-114226| CAS NO：1887014-12-1| 分子式：C₁₈H₁₅ClN₄O₂| 分子量：354.79

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-114226	￥2500.00	杭州北京（现货）
Bellancom-114226	￥3500.00	杭州北京（现货）
Bellancom-114226	￥7000.00	杭州北京（现货）
Bellancom-114226	￥11000.00	杭州北京（现货）
Bellancom-114226	￥0.00	杭州北京（现货）

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Olutasidenib FT-2102

产品介绍

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 IC₅₀ 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) .

体外研究

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice.
Dosage:	12.5, 25, and 50 mg/kg.
Administration:	Three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals.
Result:	Showed a time and dose-dependent inhibition of 2-HG levels in in tumor. At the highest dose tested in these studies (50 mg/kg), treatment with FT-2102 inhibited 2-HG levels in the tumor by >90% for up to 24 hours after the last dose in the HCT116-IDH1-R132H/+ xenograft model.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice.
Dosage:	12.5, 25, and 50 mg/kg.
Administration:	Three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals.
Result:	Showed a time and dose-dependent inhibition of 2-HG levels in in tumor. At the highest dose tested in these studies (50 mg/kg), treatment with FT-2102 inhibited 2-HG levels in the tumor by >90% for up to 24 hours after the last dose in the HCT116-IDH1-R132H/+ xenograft model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (352.32 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8186 mL	14.0928 mL	28.1857 mL
5 mM	0.5637 mL	2.8186 mL	5.6371 mL
10 mM	0.2819 mL	1.4093 mL	2.8186 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.86 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.86 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.86 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.86 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。