1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-(dimethylamino)-ethanone manufacturers
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| | 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-(dimethylamino)-ethanone Basic information |
| | 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-(dimethylamino)-ethanone Chemical Properties |
| Boiling point | 703.2±60.0 °C(Predicted) | | density | 1.33±0.1 g/cm3(Predicted) | | form | Solid | | pka | 8.24±0.28(Predicted) | | color | White to off-white |
| | 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-(dimethylamino)-ethanone Usage And Synthesis |
| Description | CHMFL-FLT3-122 is a potent and orally available FLT3 kinase inhibitor for FLT3-ITD positive acute myeloid leukemia. In vivo CHMFL-FLT3-122 significantly suppressed the tumor growth in MV4-11 cell inoculated xenograft model (50 mg/kg) without exhibiting obvious toxicity. | | Uses | CHMFL-FLT3-122 is a potent, selective and orally active FLT3 kinase with an IC50 of 40 nM. CHMFL-FLT3-122 shows selectivity for FLT3 over BTK (IC50 of 421 nM) and c-KIT (IC50 of 559 nM) kinases. CHMFL-FLT3-122 induces apoptosis by arresting the cell cycle into the G0/G1 phase[1]. | | in vivo | CHMFL-FLT3-122 (12.5-50 mg/kg; oral gavage; once a day; for 22 days) could almost completely suppress the tumor progression, and does not significantly affect the mice body weight[1]. | Animal Model: | Female nu/nu mice injected with MV4-11cells[1] | | Dosage: |
12.5 mg/kg, 25 mg/kg and 50 mg/kg | | Administration: | Oral gavage; once a day; for 22 days | | Result: | Could almost completely suppress the tumor progression. |
| | References | [1] Xixiang Li, et al. Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia. J Med Chem. 2015 Dec 24;58(24):9625-38. DOI:10.1021/acs.jmedchem.5b01611 |
| | 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-(dimethylamino)-ethanone Preparation Products And Raw materials |
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