Iadademstat dihydrochloride(Synonyms: ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride)

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Iadademstat dihydrochloride (Synonyms: ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride) 纯度: 98.30%

Iadademstat (ORY-1001) dihydrochloride 是一种不可逆的选择性赖氨酸特异性脱甲基酶 1A (KDM1A/LSD1) 抑制剂。

Iadademstat dihydrochloride(Synonyms: ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride)

Iadademstat dihydrochloride Chemical Structure

CAS No. : 1431303-72-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in Water ￥1694 In-stock
5 mg ￥1540 In-stock
10 mg ￥2450 In-stock
50 mg ￥8450 In-stock
100 mg ￥15000 In-stock
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Iadademstat dihydrochloride 相关产品

•相关化合物库:

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生物活性

Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.

IC50 & Target

KDM1A/LSD1[1]
体外研究
(In Vitro)

Iadademstat dihydrochloride is a KDM1A inhibitor that inactivate KDM1A by irreversible binding to the flavin adenine nucleotide (FAD) cofactor. Iadademstat has very high selectivity for KDM1A over the MAO enzymes, high selectivity over KDM1B and unrivaled subnanomolar cellular activity in differentiation and colony formation assays on mixed lineage leukemia (MLL)-translocated acute myeloid leukemia (AML) cell lines. Iadademstat provokes a time and dose-dependent induction of the Cd11b differentiation marker in MLL-AF9 cells, which interestingly preceeds changes in H3K4me2 levels. While MLL-translocated cells are especially sensitive, other acute leukemia (AL) cell lines also respond to Iadademstat[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.
体内研究
(In Vivo)

Iadademstat reduces AML tumor growth in mice and rat xenografts and increases survival time in a disseminated model of T-ALL[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

303.27

Formula

C15H24Cl2N2
CAS 号

1431303-72-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

H2O : 57.75 mg/mL (190.42 mM; Need ultrasonic and warming)

DMSO : 0.69 mg/mL (2.28 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2974 mL 16.4870 mL 32.9739 mL
5 mM 0.6595 mL 3.2974 mL 6.5948 mL
10 mM 0.3297 mL 1.6487 mL 3.2974 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 (sealed storage, away from moisture)。-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]. Maes T, et al. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. Epigenomics. 2015;7(4):609-26. doi: 10.2217/epi.15.9.

    [2]. Tamara Maes, et al. ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia. Cancer Cell. 2018 Mar 12;33(3):495-511.e12.

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