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PLX7904

Catalog No. T6949   CAS 1393465-84-3
Synonyms: PB04

PLX7904 (PB04), also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.

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PLX7904 Chemical Structure
PLX7904, CAS 1393465-84-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 29.00
5 mg In stock $ 50.00
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1 mL * 10 mM (in DMSO) In stock $ 54.00
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Purity: 96.27%
Purity: 96.27%
Purity: 96.27%
Purity: 96.27%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PLX7904 (PB04), also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.
Targets&IC50 BRAF:5 nM
In vitro PLX7940 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. Consistent with ERK1/2 re-activation driving the re-acquisition of malignant properties, PLX7904 promotes apoptosis and inhibits entry into S phase and anchorage-independent growth in mutant N-RAS mediated vemurafenib-resistant cells. PLX7904 is also evaluated in the human SCC cell line A431 and the human breast adenocarcinoma cell line SKBR3 as these cells achieve MAPK pathway activation by upstream signals feeding into RAS (through overexpression of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), respectively)[1][2].
In vivo PLX7904 inhibits the COLO205 xenograft growth in eight mice per group[1].
Cell Research Cells are treated with PB04(PLX7904) at different concentrations (0, 0.05, 0.1, 1, 5 μM) for 24 h. Cells are lysed and analyzed by Western blotting with phospho-MEK1/2, total MEK1/2, phospho-ERK1/2 and total ERK1/2 antibodies. (Only for Reference)
Synonyms PB04
Molecular Weight 512.53
Formula C24H22F2N6O3S
CAS No. 1393465-84-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 100 mg/mL (195.11 mM)

TargetMolReferences and Literature

1. Zhang C, et al. Nature. 2015, 526(7574):583-586. 2. Le K, et al. Pigment Cell Melanoma Res. 2013, 26(4):509-517.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Anti-Prostate Cancer Compound Library Inhibitor Library Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compounds Library Max Anti-Liver Cancer Compound Library Anti-Colorectal Cancer Compound Library Bioactive Compound Library Kinase Inhibitor Library

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Keywords

PLX7904 1393465-84-3 MAPK Raf PB04 Inhibitor inhibit PB-04 Raf kinases PLX-7904 PB 04 PLX 7904 inhibitor

 

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