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PLX7904

Cat. No. M9008
PLX7904 Structure
Synonym:

PB04

Size Price Availability Quantity
5mg USD 165 In stock
10mg USD 300 In stock
50mg USD 1350 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

PLX7904 is a potent and selective BRAF inhibitor, with IC50 of appr 5 nM against BRAFV600E in mutant RAS expressing cells. PLX7904 potently inhibit ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. PLX7904 potently inhibits phosphorylation of ERK1/2 in mutant BRAF melanoma cells without eliciting paradoxical activation in wild-type BRAF, mutant NRAS melanoma cells.

In vivo, PLX7904 inhibits the COLO205 xenograft growth in eight mice per group.

Protocol
Cell Experiment
Cell lines WM793, WM115, WM9, WM278, WM1346, WM1366, WM1361A, Sbcl2, 1205Lu, A375, SK-MEL 24, SKMEL-2, and SK-MEL 207 cells
Preparation method Cells are treated with 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.
Concentrations 0, 0.05, 0.1, 1, 5 μM
Incubation time 24 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 512.53
Formula C24H22F2N6O3S
CAS Number 1393465-84-3
Purity >98%
Solubility DMSO: ≥ 40 mg/mL
Storage at -20°C
References

RAF inhibitors that evade paradoxical MAPK pathway activation.
Zhang C, et al. Nature. 2015 Oct 22;526(7574):583-6. PMID: 26466569.

Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors.
Basile KJ, et al. Pigment Cell Melanoma Res. 2014 May;27(3):479-84. PMID: 24422853.

Selective RAF inhibitor impairs ERK1/2 phosphorylation and growth in mutant NRAS, vemurafenib-resistant melanoma cells.
Le K, et al. Pigment Cell Melanoma Res. 2013 Jul;26(4):509-17. PMID: 23490205.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PLX7904, PB04 supplier, Raf, inhibitors

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