PLX4032 (Vemurafenib)

Catalog No.: A10739

Raf inhibitor

PLX4032 (Vemurafenib)

PLX4032 (Vemurafenib) Chemical Structure

CAS NO. 918504-65-1

PLX4032 (Vemurafenib) also known as RG7204, Vemurafenib, R7204; RO5185426. PLX4032 is a B-raf inhibitor with an IC50 of 44 nM.

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10 mg

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50 mg

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100 mg

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200 mg

Regular Price: $200.00

Special Price $160.00

10mM * 1mL in DMSO

Regular Price: $50.00

Special Price $40.00

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  • Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
  • Jan Dorrie, .et al. BRAF and MEK Inhibitors Influence the Function of Reprogrammed T Cells: Consequences for Adoptive T-Cell Therapy, Int J Mol Sci, 2018, Jan; 19(1): 289 PMID: 29346301
  • Kudo K, .et al. Cell surface CD63 increased by up-regulated polylactosamine modification sensitizes human melanoma cells to the BRAF inhibitor PLX4032, FASEB J, 2018, Dec 3:fj201800664RR PMID: 30508500
  • Min Ho Choe, .et al. miR-550a-3-5p acts as a tumor suppressor and reverses BRAF inhibitor resistance through the direct targeting of YAP, Cell Death Dis, 2018, Jun; 9(6): 640 PMID: 29844307
  • Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
  • Aishwarya Kundu, .et al. Inhibition of Oncogenic BRAF Activity by Indole-3-Carbinol Disrupts Microphthalmia-Associated Transcription Factor Expression and Arrests Melanoma Cell Proliferation, Mol Carcinog, 2017, Jan; 56(1): 49-61 PMID: 26878440
  • Toshinori Sueda, .et al. BRAFV600E inhibition stimulates AMP-activated protein kinase-mediated autophagy in colorectal cancer cells, Sci Rep, 2016, 6: 18949 PMID: 26750638
  • Yanling Li, .et al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells, Onco Targets Ther, 2015, 8: 1043-1051 PMID: 25999739

Biological Activity

PLX4032 (Vemurafenib) also known as RG7204, Vemurafenib, R7204; RO5185426. PLX4032 is a B-raf inhibitor with an IC50 of 44 nM.
Targets
Target Value
SRMSIC50: 18nM
ACK1IC50: 19nM
B-Raf(V600E)IC50: 31nM
C-RafIC50: 48nM
MAP4K5(KHS1)IC50: 51nM
FGRIC50: 63nM
B-RafIC50: 100nM
LCKIC50: 183nM
BRKIC50: 213nM
NEK11IC50: 317nM
BLKIC50: 547nM
LynBIC50: 599nM
YES1IC50: 604nM
WNK3IC50: 877nM
MNK2IC50: 1.717μM
FRK(PTK5)IC50: 1.884μM
CSKIC50: 2.339μM
SrcIC50: 2.389μM
In vitro (25°C) DMSO 83 mg/mL (169.41 mM)
Water Insoluble
Ethanol Insoluble
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O (suspension) 4 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 20.41 mL 102.06 mL 204.12 mL
0.5 mM 4.08 mL 20.41 mL 40.82 mL
1 mM 2.04 mL 10.21 mL 20.41 mL
5 mM 0.41 mL 2.04 mL 4.08 mL

*The above data is based on the productmolecular weight 489.9 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Catalog Num A10739
Actions Inhibitor
CAS No. 918504-65-1
Formula C23H18ClF2N3O3S
M. Wt 489.9
Solubility DMSO
Purity >98%
Synonyms RG7204,RO5185426,Zelboraf, PLX-4032
SMILES CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=NC=C(C=C23)C4=CC=C(C=C4)Cl)F
Storage

Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for 36 months.
In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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