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Vemurafenib (PLX4032)

Catalog No.
C007B-306808
Mfr. No.
V409259-1ml
Mfr. Name
Aladdin Scientific
Qty/UOM
1
UOM
EA
Price: $183.29
List Price: $203.65

InformationIn vitroPLX4032 inhibits B-RAFV600E, C-RAF, as well as wildtype B-RAF, with IC50 of 31 nM, 48 nM and 100 nM, respectively. PLX4032 also inhibits several non-RAF kinases, including ACK1, KHS1, and SRMS, with IC50 of 18 nM to 51 nM. In

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InformationIn vitroPLX4032 inhibits B-RAFV600E, C-RAF, as well as wildtype B-RAF, with IC50 of 31 nM, 48 nM and 100 nM, respectively. PLX4032 also inhibits several non-RAF kinases, including ACK1, KHS1, and SRMS, with IC50 of 18 nM to 51 nM. In melanoma cell lines, the inhibitory effect by PLX4032 depends on B-RAF mutational status, because PLX4032 potently inhibits those harboring B-RAF V600 mutants, including V600E, V600D, V600K, and V600R, but not wildtype or other mutants. The IC50 values of PLX4032 on these cells, including MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058, ranges from 20 nM to 1 μM. In these cells, PLX4032 (0.1 μM to 30 μM) also inhibits the phosphorylation of both MEK1/2 and ERK1/2. PLX4032 is highly effective in the treatment of melanoma, for its ability of inhibiting B-RAFV600E. However, PLX4032 displays limited effect in colon cancer patients that also carrying B-RAFV600E oncoprotein. The reason for this is that, in colon cancer cells, B-RAFV600E inhibition by PLX4032 results in a rapid feedback EGFR activation, which compensates for the PLX4032-inhibited cell proliferation.In vivoIn B-RAFV600E-mutant mice xenograft models, PLX4032 (6 mg/kg–20 mg/kg) inhibits tumor growth. In mice xenograft models of LOX, Colo829, and A375 cells, PLX4032 (12.5 mg/kg–100 mg/kg) inhibits tumor growth and prolongs mice survival.Cell Datacell lines:Concentrations:0–10 μM , dissolved in DMSOIncubation Time:5 daysPowder Purity:≥97%. Specification: 10mM in DMSO Molecular Formula: C23H18ClF2N3O3S Molecular Weight: 489.92
UPC:
51311810
Condition:
New
Availability:
2 weeks
Weight:
0.85 Ounces
HazmatClass:
No
WeightUOM:
LB
MPN:
V409259-1ml
CAS:
918504-65-1
Product Size:
1ml

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