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553015

Sigma-Aldrich

Raf Kinase Inhibitor V - CAS 918505-84-7 - Calbiochem

The Raf Kinase Inhibitor V, also referenced under CAS 918505-84-7, controls the biological activity of Raf Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

Raf Kinase Inhibitor V - CAS 918505-84-7 - Calbiochem, Propane-1-sulfonic acid-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl)-amide, PLX4720

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About This Item

Empirical Formula (Hill Notation):
C17H14ClF2N3O3S
CAS Number:
Molecular Weight:
413.83
UNSPSC Code:
12352200

Pricing and availability is not currently available.

Quality Level

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange-yellow

solubility

DMSO: 100 mg/mL
ethanol: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

General description

A cell-permeable azaindole compound that interacts with Raf via both the ATP-binding site and a "Raf-selective pocket" that exhibits conformation-dependent inhibitor-binding modes and accounts for the compound′s preferential binding and inhibitory activity toward the active Raf mutants (IC50 = 6.7, 13, 130, 160, and >1,300 nM against C-Raf-1Y340D/Y341D, B-RafV600E, BRK, WT B-Raf, and 64 other kinases, respectively). Shown to inhibit the proliferation and cellular Erk phosphorylation much more potently in B-RafV600E-bearing than WT B-Raf-bearing cancer cell lines in vitro and effectively suppress COLO205-derived tumor growth in mice in vivo (near complete regression during the 1-wk treatment period; 20 mg/kg, daily p.o.).
A cell-permeable azaindole compound that interacts with Raf via both the ATP-binding site and a "Raf-selective pocket" that exhibits conformation-dependent inhibitor-binding modes and accounts for the compound′s preferential binding and inhibitory activity toward the active Raf mutants (IC50 = 6.7, 13, 130, 160, and >1,300 nM against C-Raf-1Y340D/Y341D, B-RafV600E, BRK, WT B-Raf, and 64 other kinases, respectively). Shown to inhibit the proliferation and cellular Erk phosphorylation much more potently in B-RafV600E-bearing than WT B-Raf-bearing cancer cell lines in vitro and effectively suppress COLO205-derived tumor growth in mice in vivo (near complete regression during the 1-wk treatment period; 20 mg/kg, daily, p.o.).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Tsai, J., et al. 2008. Proc. Natl. Acad. Sci. USA105, 3041.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


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    Gang Cheng et al.
    Cancer treatment and research communications, 25, 100210-100210 (2020-09-29)
    Melanoma is an aggressive form of skin cancer for which there are no effective drugs for prolonged treatment. The existing kinase inhibitor antiglycolytic drugs (B-Raf serine/threonine kinase or BRAF inhibitors) are effective for a short time followed by a rapid

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