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DDP-38003 trihydrochloride Sale

目录号 : GC34296

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

DDP-38003 trihydrochloride Chemical Structure

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,548.00
现货
1mg
¥810.00
现货
5mg
¥1,530.00
现货
10mg
¥2,610.00
现货
50mg
¥9,900.00
现货
100mg
¥9,179.00
现货

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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 trihydrochloride 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. SDF
Canonical SMILES [H]Cl.[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 C21H29Cl3N4O 分子量 459.84
溶解度 DMSO : ≥ 120 mg/mL (260.96 mM) 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.1747 mL 10.8733 mL 21.7467 mL
5 mM 0.4349 mL 2.1747 mL 4.3493 mL
10 mM 0.2175 mL 1.0873 mL 2.1747 mL
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