[CAS NO. 1393465-84-3] PLX7904

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PRODUCTS SPECIFICATIONS [1393465-84-3]

Catalog

HY-18997

Brand

MCE

CAS

1393465-84-3

DESCRIPTION [1393465-84-3]

Overview

MDL	MFCD29472265
Molecular Weight	512.53
Molecular Formula	C24H22F2N6O3S
SMILES	O=S(NC1=CC=C(F)C(C(C2=CNC3=NC=C(C4=CN=C(C5CC5)N=C4)C=C32)=O)=C1F)(N(CC)C)=O

For research use only. We do not sell to patients.

3 Publications Citing Use of MCE

Summary

PLX7904 is a potent and selective BRAF inhibitor, with IC ₅₀ of appr 5 nM against BRAF ^V600E in mutant RAS expressing cells.

IC50 & Target

BRaf ^V600E

5 nM (IC ₅₀ , in mutant RAS expressing cells)

In Vitro

PLX7904 inhibits the in vitro growth of two melanoma cell lines (A375 and COLO829) and an additional human colorectal cancer cell line COLO205 that expresses BRAF ^V600E with IC ₅₀ values of 0.17 μM, 0.53 μM, and 0.16 μM, respectively, on a par with vemurafenib IC ₅₀ values in the same assays (0.33 μM, 0.69 μM, and 0.25 μM, respectively) ^[1] . PLX7904 and PLX8394 potently inhibit ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. PLX7904 and PLX8394 treatment at 1 μM concentration reduce colony formation and viability in parental cells to a similar level as PLX4720 ^[2] . PPLX7904 potently inhibits phosphorylation of ERK1/2 in mutant BRAF melanoma cells without eliciting paradoxical activation in wild-type BRAF, mutant NRAS melanoma cells. PPLX7904 inhibits ERK1/2 in PLX470-resistant cell lines. PPLX7904 treatment promotes apoptosis and inhibits anchorage-independent growth of vemurafenib resistant cells ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 30 mg/mL ( 58.53 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9511 mL	9.7555 mL	19.5111 mL
5 mM	0.3902 mL	1.9511 mL	3.9022 mL
10 mM	0.1951 mL	0.9756 mL	1.9511 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution

* All of the co-solvents are available by MCE.