Share this post on:

product name PLX-4720


Description: PLX4720, a 7-azaindole derivative discovered by a structure-guided discovery approach, is a selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, it is 10-fold more selective for B-RafV600E than wild-type B-Raf.PLX-4720 potently inhibits ERK phosphorylation in tumor cell lines harboring B-RafV600E, induces cell cycle arrest and apoptosis in B-RafV600E-positive melanoma cells and causes tumor growth delays in B-RafV600E-dependent tumor xenograft models through oral administration.

References: Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6.



Molecular Weight (MW)

413.83
Formula

C17H14ClF2N3O3S
CAS No.

918505-84-7
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 83 mg/mL (200.6 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL
Solubility (In vivo)

2% DMSO+50% PEG 300+5% Tween 80+ddH2O: 5 mg/mL

other peoduct :

General Oral administration of PLX-4720 at 20 mg/kg/day induces significant tumor growth delays and regressions in B-RafV600E-dependent COLO205 tumor xenografts, without obvious adverse effects in mice even at dose of 1 g/kg.
Animal model Female athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells
Formulation  Suspended in vehicle (5% DMSO, 1% methylcellulose)
Dosages 5, 20, or 100 mg/kg
Administration  Administered orally once or twice daily
Reference [1] Tsai J, et al. Proc Natl Acad Sci U S A, 2008, 105(8), 3041-3046.

Vipadenant