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ML390

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Chemical Structure| 2029049-79-2 同义名 : -
CAS号 : 2029049-79-2
货号 : A589360
分子式 : C21H21F3N2O3
纯度 : 99%+
分子量 : 406.398
MDL号 : MFCD30489750
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(61.52 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Dehydrogenase

    DHODH, IC50:0.56 μM
描述 Dihydroorotate dehydrogenase (DHODH) catalyzes the oxidation of dihydroorotate to orotate in de novo pyrimidine synthesis, e.g., uridine 5′-monophosphate. ML390 is a small-molecule probe active in overcoming differentiation arrest in a model of AML (acute myeloid leukemia). Its effect is due to inhibition of DHODH-catalyzed pyrimidine synthesis[3]. ML390 is very well-tolerated with limited cytotoxicity at high concentration when assayed against cultures of normal human primary bone marrow cells. ML390 triggers myeloid differentiation in murine and human cell line models of acute myeloid leukemia. The stability of probe ML390 in PBS (0.1% DMSO) was measured and the probe is stable as approximately 100% was present after 24 hours of incubation[4].
作用机制 The (R)-amino tetralin group of ML390 is located within the innermost part of the cavity and makes the closest contact[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.61mL

4.92mL

2.46mL
参考文献

[1]Lewis TA, Sykes DB, et al. Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ACS Med Chem Lett. 2016 Sep 28;7(12):1112-1117.

[2]Sykes DB, Haynes MK, et al. Discovering Small Molecules that Overcome Differentiation Arrest in Acute Myeloid Leukemia. 2013 Dec 15 [updated 2015 Feb 11] .

[3]Lewis TA, Sykes DB, Law JM, et al. Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ACS Med Chem Lett. 2016;7(12):1112‐1117

[4]Sykes DB, Haynes MK, Waller A, et al. Discovering Small Molecules that Overcome Differentiation Arrest in Acute Myeloid Leukemia. In: Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD): National Center for Biotechnology Information (US); 2010