1070690-06-0
1070690-06-0 structure
- Name: HMS-101
- Chemical Name: 2-{2-[3-(4-Fluorophenyl)-1-pyrrolidinyl]ethyl}-1,4-dimethylpiperazine
- CAS Number: 1070690-06-0
- Molecular Formula: C18H28FN3
- Molecular Weight: 305.433
- Create Date: 2020-01-11 19:30:51
- Modify Date: 2024-04-01 14:29:12
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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.
| Name | 2-{2-[3-(4-Fluorophenyl)-1-pyrrolidinyl]ethyl}-1,4-dimethylpiperazine |
|---|---|
| Synonyms |
Piperazine, 2-[2-[3-(4-fluorophenyl)-1-pyrrolidinyl]ethyl]-1,4-dimethyl-
2-{2-[3-(4-Fluorophenyl)-1-pyrrolidinyl]ethyl}-1,4-dimethylpiperazine MFCD30726281 |
| 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) |
| 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 |