FN-1501
FN-1501 Basic information
- Product Name:
- FN-1501
- Synonyms:
-
- 1H-Pyrazole-3-carboxamide, N-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-4-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-
- 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide
- FN-1501, 10 mM in DMSO
- CAS:
- 1429515-59-2
- MF:
- C22H25N9O
- MW:
- 431.49
- Mol File:
- 1429515-59-2.mol
FN-1501 Chemical Properties
- Density
- 1.427±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 50 mg/mL (115.88 mM)
- form
- Solid
- pka
- 11.73±0.70(Predicted)
- color
- White to off-white
FN-1501 Usage And Synthesis
Uses
FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.
in vivo
FN-1501 exhibits potent antitumor activity, and shows little cytotoxicity on normal lymphocyte cells, with LD50 of 185.67 mg/kg in ICR mice. FN-1501 (15. 30, or 40 mg/kg/d, i.v.) dose-dependently and significantly suppresses the growth of tumor in MV4-11-cell-inoculated-xenograft mice[1].
IC 50
Cdk4/cyclin D1: 0.85 nM (IC50); CDK6/cyclinD1: 1.96 nM (IC50); cdk2/cyclin A: 2.47 nM (IC50); FLT3: 0.28 nM (IC50)
References
[1] Wang Y, et al. Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. J Med Chem. 2018 Feb 22;61(4):1499-1518. DOI:10.1021/acs.jmedchem.7b01261
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