Free shipping on all orders over $ 500

PLX7904

Cat. No. M9008
PLX7904 Structure
Synonym:

PB04

Size Price Availability Quantity
5mg USD 165  USD165 In stock
10mg USD 300  USD300 In stock
50mg USD 1350  USD1350 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 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

[1] Zhang C, et al. Nature. RAF inhibitors that evade paradoxical MAPK pathway activation.

[2] Basile KJ, et al. Pigment Cell Melanoma Res. Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors.

[3] Le K, et al. Pigment Cell Melanoma Res. Selective RAF inhibitor impairs ERK1/2 phosphorylation and growth in mutant NRAS, vemurafenib-resistant melanoma cells.

Related Raf Products
LY3009120

LY3009120 (DP-4978) is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively.

AZ304

AZ304 is a potent dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF with IC50 values of 79 nM and 38 nM respectively.

Lifirafenib (BGB-283)

Lifirafenib (BGB-283) is a novel potent and selective RAF Kinase and EGFR inhibitor with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.

BI 882370

BI 882370 is a highly potent and selective RAF inhibitor that binds to the DFG-out (inactive) conformation of the BRAF kinase.

Naporafenib

Naporafenib (also known as LXH254) is an orally available inhibitor of C-Raf and B-Raf with potential antineoplastic activity.

  Catalog
Abmole Inhibitor Catalog




Keywords: PLX7904, PB04 supplier, Raf, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.