HMS-101

Names

[ Name ]:
HMS-101

[Synonym ]:
Piperazine, 2-[2-[3-(4-fluorophenyl)-1-pyrrolidinyl]ethyl]-1,4-dimethyl-
2-{2-[3-(4-Fluorophenyl)-1-pyrrolidinyl]ethyl}-1,4-dimethylpiperazine
MFCD30726281

Biological Activity

[Description]:

HMS-101 (HMS101) is a potent, selective mutant IDH1 inhibitor, the IC50 is significantly lower in mouse bone marrow cells transduced with IDH1mut compared with IDH1wt (1 uM vs 12 uM, respectively); binds to the isocitrate-binding pocket of mutant IDH1, significantly reduces intracellular R-2HG levels in vitro HoxA9+IDH1mut cells at 10 uM; induces apoptosis in IDH1mut cells, markedly reduces phospho-ERK1/2 and the ratio of phospho-ERK/total-ERK, inhibits human AML cell growth.

[References]

References 1. Chaturvedi A, et al. Blood. 2013 Oct 17;122(16):2877-87. View Related Products by Target Isocitrate Dehydrogenase (IDH)

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
395.2±42.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₈H₂₈FN₃

[ Molecular Weight ]:
305.433

[ Flash Point ]:
192.8±27.9 °C

[ Exact Mass ]:
305.226715

[ LogP ]:
1.75

[ Vapour Pressure ]:
0.0±0.9 mmHg at 25°C

[ Index of Refraction ]:
1.524

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.