2040295-03-0
2040295-03-0 structure
- Name: Pexidartinib hydrochloride (PLX-3397)
- Chemical Name: Pexidartinib hydrochloride
- CAS Number: 2040295-03-0
- Molecular Formula: C20H16Cl2F3N5
- Molecular Weight: 454.28
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK c-Fms
- Create Date: 2019-06-05 07:44:48
- Modify Date: 2024-01-12 12:56:42
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Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases, such as FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1) and NTRK3 (TRKC), with IC50s of 160, 350, 860, 880, and 890 nM, respectively[1].
| Name | Pexidartinib hydrochloride |
|---|
| Description | Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases, such as FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1) and NTRK3 (TRKC), with IC50s of 160, 350, 860, 880, and 890 nM, respectively[1]. |
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| Related Catalog | |
| Target |
IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM (NTRK3)[1] |
| In Vivo | Pexidartinib (PLX3397; 0.25, 1 mg/kg, i.p., twice daily for 8 days) inhibits the proliferation of microglia and BrdU-positive cells in neonatal mice[2]. Pexidartinib (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice[2]. Animal Model: Neonatal mice[2] Dosage: 0.25, 1 mg/kg Administration: I.P. twice daily for 8 days Result: Decreased the number of microglia and BrdU-positive proliferative cells, but did not change the cleaved caspase-3-positive cells. |
| References |
| Molecular Formula | C20H16Cl2F3N5 |
|---|---|
| Molecular Weight | 454.28 |
| Storage condition | 2-8℃ |