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DDP-38003 dihydrochloride Sale

目录号 : GC33013

DDP-38003dihydrochloride是新颖有口服活性的KDM1A/LSD1抑制剂,IC50值为84nM。

DDP-38003 dihydrochloride Chemical Structure

Cas No.:1831167-98-6

规格 价格 库存 购买数量
1mg
¥810.00
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5mg
¥1,710.00
现货
10mg
¥3,150.00
现货
50mg
¥11,700.00
现货
100mg
¥17,100.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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实验参考方法

Animal experiment:

Mice: CD-1 mice is used in the study. DDP-38003 is dissolved (40% PEG 400 in a 5% glucose solution) and orally administered 3 days per week (Monday, Tuesday and Wednesday) for 3 weeks at the doses of 11.25 mg/kg and 22.5 mg/kg. The treatment started once blast cells are detected in the recipients' peripheral blood (10 days after cell injection). The survival of mice of the different experimental groups is analyzed and represented by a Kaplan-Meier survival plot[1].

References:

[1]. Vianello P, et al. Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent. J Med Chem. 2016 Feb 25;59(4):1501-17.

产品描述

DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.

DDP-38003 inhibits KDM1A with an IC50 of 84 nM. DDP-38003 is more active in reducing the colony forming ability and in inducing thedifferentiation of THP-1 cells compared to the 1R, 2S analogue[1].

DDP-38003 exhibits in vivo efficacy after oral administration, determining a 62% increased survival in mouse leukemia models with evidence of KDM1A inhibition. The half life of DDP-38003 is 8 h. A significant dose dependent increase of mice survival is obtained by DDP-38003 treatment. The survival rate increases 35% and 62% at the dose of 11.25 and 22.50 mg/kg, respectively. DDP-38003 is a potential oral anticancer agent[1].

[1]. Vianello P, et al. Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent. J Med Chem. 2016 Feb 25;59(4):1501-17.

Chemical Properties

Cas No. 1831167-98-6 SDF
Canonical SMILES [H]Cl.O=C(NC1=CC=C([C@@H]2C[C@H]2N)C=C1)C(C=C3)=CC=C3N4CCN(C)CC4.[H]Cl
分子式 C21H28Cl2N4O 分子量 423.38
溶解度 DMSO : ≥ 29 mg/mL (68.50 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-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。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.3619 mL 11.8097 mL 23.6194 mL
5 mM 0.4724 mL 2.3619 mL 4.7239 mL
10 mM 0.2362 mL 1.181 mL 2.3619 mL
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