PLX-4720 | CAS 918505-84-7

PLX-4720

This product is for research use only, not for human use. We do not sell to patients.

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500mg	$430	Check With Us
1g	$645	Check With Us
5g	$1630	Check With Us

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Cat #: V1002 CAS #: 918505-84-7 Purity ≥ 98%

Description: PLX4720 (PLX-4720; PLX 4720), a 7-azaindole/pyrrolopyridine-based vemurafenib derivative discovered by a structure-guided discovery approach, is a novel, potent and selective inhibitor of B-RafV600E mutant with potential antitumor activity.

References: Tsai J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A, 2008, 105(8), 3041-3046.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	413.83
Molecular Formula	C17H14ClF2N3O3S
CAS No.	918505-84-7
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 83 mg/mL (200.6 mM)r
	Water: <1 mg/mL (slightly soluble or insoluble)r
	Ethanol: <1 mg/mL
Solubility In Vivo	2% DMSO+50% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
SMILES Code	CCCS(=O)(NC1=CC=C(F)C(C(C2=CNC3=NC=C(Cl)C=C32)=O)=C1F)=O
Synonyms	PLX 4720; PLX4720; PLX-4720

Protocol	In Vitro	PLX-4720 displays >10 times selectivity against wild type B-Raf, and >100 times selectivity over other kinases such as Frk, Src, Fak, FGFR, and Aurora A with IC50 of 1.3-3.4 μM. PLX-4720 significantly inhibits the ERK phosphorylation in cell lines bearing B-RafV600E with IC50 of 14-46 nM, but not the cells with wild-type B-Raf. PLX-4720 significantly inhibits the growth of tumor cell lines bearing the B-RafV600E oncogene, such as COLO205, A375, WM2664, and COLO829 with GI50 of 0.31 μM, 0.50 μM, 1.5 μM, and 1.7 μM, respectively. In addition, PLX-4720 treatment at 1 μM induces cell cycle arrest and apoptosis exclusively in the B-RafV600E-positive 1205Lu cells, but not in the B-Raf wild-type C8161 cells.
Protocol	In Vivo	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. PLX-4720 at 100 mg/kg twice daily almost completely eliminates the 1205Lu xenografts bearing B-RafV600E, while has no activity against C8161 xenografts bearing wild-type B-Raf. The anti-tumor effects of PLX-4720 correlate with the blockade of MAPK pathway in those cells harboring the V600E mutation.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.4165 mL	12.0823 mL	24.1645 mL	48.3290 mL
5mM	0.4833 mL	2.4165 mL	4.8329 mL	9.6658 mL
10mM	0.2416 mL	1.2082 mL	2.4165 mL	4.8329 mL
20mM	0.1208 mL	0.6041 mL	1.2082 mL	2.4165 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.