PLX-4032 Inhibitor CAS No. 918504-65-1

Cat. No.	Name	Size	Price
KI0354	PLX-4032	10 mg	$120
	PLX-4032	50 mg	$513
	PLX-4032	500 mg	$3080

Chemical Characteristic

Product Name	PLX-4032
Synonyms	RG7204, RO5185426, Vemurafenib, Zelboraf
CAS No.	918504-65-1
Molecular Weight	489.92
Formula	C₂₃H₁₈ClF₂N₃O₃S
Chemical Name	N-?[3-?[[5-?(4-?chlorophenyl)?-?1H-?pyrrolo[2,?3-?b]?pyridin-?3-?yl]?carbonyl]?-?2,?4-?difluorophenyl]?-1-?propanesulfonamide
Smiles	C(CC)S(=O)(=O)Nc1c(c(c(cc1)F)C(=O)c1c2c(ncc(c2)c2ccc(cc2)Cl)[nH]c1)F
Chemical Structure

Biological activities

PLX-4032 is a potent small-molecule B-Raf inhibitor for the potential treatment of malignant melanoma. PLX-4032 inhibits B-RaF^V600E with an IC50 of 30 nM. PLX-4032 possesses 3-fold selectivity for the V600E mutation over the wild-type kinase. ^[1] PLX-4032 inhibits the activity of B-Raf with an IC50 of 100 nM. In addition, PLX-4032 also prevents C-Raf. The IC50 of PLX-4032 against C-Raf is 48 nM. In contrast, PLX-4032 blocks SRMS (src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites), ACK1 (activated cdc42-associated kinase), MAP4K5 (mitogen-activated protein kinase kinase kinase kinase 5) and FGR with IC50 of 18, 19, 51 and 63 nM, respectively. ^[2] PLX-4032 inhibits the growth of B-RaF^V600E-positive melanoma cell lines both in vitro and in vivo. PLX-4032 potently inhibits proliferation and mitogen-activated protein/extracellular signal-regulated kinase (MAPK/ERK) kinase and ERK phosphorylation in a panel of tumor cell lines, including melanoma cell lines expressing B-RaF^V600E or other mutant B-Raf proteins altered at codon 600. In contrast, PLX-4032 lacks activity in cell lines that express wild-type B-Raf or non-V600 mutations. PLX-4032 treatment gives rise to partial or complete tumor regressions and improved animal survival, in a dose-dependent manner. PLX-4032 also potently inhibits proliferation of melanoma cell lines expressing other codon 600 B-Raf mutations (V600D, V600K, and V600R). In addition, proliferation of the WM1789 melanoma cell line expressing B-Raf^K601E is moderately inhibited by PLX-4032. PLX-4032 inhibits the phosphorylation of MEK and ERK in the two representative B-RaF^V600E-expressing melanoma cell lines, Colo829 and LOX. PLX-4032 also blocks MEK and ERK phosphorylation in the WM2664 and WM1341D cell lines, which expresses B-RafV600D and B-Raf^V600R, respectively. ^[1] PLX-4032 inhibits A375 cells, ARO cells, and NPA cells with IC50 values of 47, 205 and 126 nM, respectively. PLX4032 inhibits TPCI cells with an IC50 of 10.77 μM. ^[3] PLX-4032 not only increases the rate of proliferation of growth factor-dependent NRAS Q61L mutant primary melanoma cells but also reduces cell adherence and increases mobility of cells from advanced lesions. ^[4] PLX-4032 significantly inhibits tumor growth and induces tumor regression. PLX-4032 significantly increases survival relative to vehicle in a dose-responsive manner. Compared with animals in the vehicle group, PLX-4032-treated mice reveal a 61% increased life span. ^[1]

Protocols

PLX-4032 is dissolved in DMSO.^[2]

References

[1] Yang H, et al. RG7204 (PLX-4032), a selective BRAF^V600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res. 2010, 70(13): 5518-5527. [2] Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature. 2010, 467(7315): 596-599. [3] Sala E, et al. BRAF silencing by short hairpin RNA or chemical blockade by PLX-4032 leads to different responses in melanoma and thyroid carcinoma cells. Mol Cancer Res. 2008, 6(5): 751-759. [4] Halaban R, et al. PLX-4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells. nt Cell Melanoma Res. 2010, 23(2): 190-200.

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