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Vemurafenib (PLX4032, RG7204)

In stock
Catalog No.
A3004
BRAF kinase inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
10mg
$50.00
In stock
50mg
$120.00
In stock
200mg
$300.00
In stock
500mg
$440.00
In stock
1000mg
$1,000.00
In stock

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Email: [email protected]

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Background

Vemurafenib is an inhibitor of BRAF kinase. It inhibits BRAFV600E and also has inhibitory activity in vitro against several other kinds of kinases, including CRAF, ARAF and wild-type BRAF. Vemurafenib is a competitive small-molecule serine–threonine kinase inhibitor that functions by binding to the ATP-binding domain of mutant BRAF. Vemurafenib can also give rise to activation of downstream MEK by normal RAF homo- and heterodimers in non-BRAF mutated cells, which has been shown to be caused by transactivation of the nondrug-bound partner in BRAF to CRAF heterodimers and CRAF to CRAF homodimers.

Reference

Keith. T Flaherty, Uma Yasothan and Peter Kirkpatrick. Vemurafenib. Nature Reviews Drug Discovery. 2011; 10: 811 – 812.

Jason J. Luke, F. Stephen Hodi. Vemurafenib and BRAF Inhibition: A New Class of Treatment for Metastatic Melanoma. Clinical Cancer Research. 2012; 18: 9 – 14.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt489.93
Cas No.918504-65-1
FormulaC23H18ClF2N3O3S
SynonymsVemurafenib,Zelboraf,PLX-4032,RG7204,RO5185426,
Solubility≥24.5mg/mL in DMSO
Chemical NameN-[3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]propane-1-sulfonamide
SDFDownload SDF
Canonical SMILESCCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=NC=C(C=C23)C4=CC=C(C=C4)Cl)F
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment:

Cell lines

MALME-3M melanoma cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

24 h; 10 μM

Applications

In melanoma cell lines, RG7204 was a potent inhibitor of proliferation in those expressing BRAFV600E but not BRAFWT. RG7204 also potently inhibited proliferation of melanoma cell lines expressing other codon 600 BRAF mutations (V600D, V600 K, and V600R).

Animal experiment:

Animal models

Athymic nude mice

Dosage form

100 mg/kg bid; oral taken.

Applications

In mice bearing Colo829 tumor xenografts, RG7204 at 100 mg/kg bid for 21 days showed greatly improved antitumor activity compared both with vehicle (P = 0.001) at the end of the study on day 38 after the tumor cell implant. There was complete tumor regression in all 10 mice treated with RG7204 by the end of the study. Survival in the mice treated with RG7204 was significantly better than in those treated with vehicle (P = 0.0008).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Yang H, Higgins B, Kolinsky K, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models[J]. Cancer research, 2010, 70(13): 5518-5527.

Biological Activity

Description Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM.
Targets B-RafV600E C-Raf MAP4K5 (KHS1) SRMS ACK1 FGR
IC50 31 nM 48 nM 51 nM 18 nM 19 nM 63 nM

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