PLX-4720

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PLX-4720

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	918505-84-7
规格:	≥98%

包装与价格：

产品介绍

理化性质和储存条件

Molecular Weight (MW)	413.83
Formula	C17H14ClF2N3O3S
CAS No.	918505-84-7
Storage	-20℃ for 3 years in powder form
Storage	-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 info	Synonym: PLX 4720; PLX4720; PLX-4720. IUPAC/Chemical Name: N-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide InChi Key: YZDJQTHVDDOVHR-UHFFFAOYSA-N InChi Code: InChI=1S/C17H14ClF2N3O3S/c1-2-5-27(25,26)23-13-4-3-12(19)14(15(13)20)16(24)11-8-22-17-10(11)6-9(18)7-21-17/h3-4,6-8,23H,2,5H2,1H3,(H,21,22) SMILES Code: CCCS(=O)(NC1=CC=C(F)C(C(C2=CNC3=NC=C(Cl)C=C32)=O)=C1F)=O

实验参考方法

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.

生物活性

Antimetastatic effects of PLX4720 require NK cells. Cancer Res; 74(24); 7298–308, 2014

PLX4720 requires perforin and CD226 for optimal antimetastatic activity.

qPCR analysis showing that PLX4720 (3μM) alters the expression of XBP1s mRNA.