PLX4032 (Vemurafenib)

Catalog No. A10739

PLX4032(Vemurafenib)也称为RG7204，Vemurafenib，R7204，RO5185426。PLX4032是B-raf抑制剂，IC50为44 nM。

Product Citations

Lee YJ, .et al. Overexpression of Dock180 and Elmo1 in melanoma is associated with cell survival and migration, Research Square, 2022, April 27th
Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
Guixin Zhu, .et al. TRIM15 and CYLD regulate ERK activation via lysine-63-linked polyubiquitination, Nat Cell Biol, 2021, Sep;23(9):978-991 PMID: 34497368
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
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
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
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
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
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

Technical details

Catalog Num	A10739
M. Wt	489.9
Formula	C23H18ClF2N3O3S
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	918504-65-1
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

Biological Activity

PLX4032(Vemurafenib)也称为RG7204，Vemurafenib，R7204，RO5185426。PLX4032是B-raf抑制剂，IC50为44 nM。

Targets

Target	Value
SRMS	IC50: 18nM
ACK1	IC50: 19nM
B-Raf(V600E)	IC50: 31nM
C-Raf	IC50: 48nM
MAP4K5(KHS1)	IC50: 51nM
FGR	IC50: 63nM
B-Raf	IC50: 100nM
LCK	IC50: 183nM
BRK	IC50: 213nM
NEK11	IC50: 317nM
BLK	IC50: 547nM
LynB	IC50: 599nM
YES1	IC50: 604nM
WNK3	IC50: 877nM
MNK2	IC50: 1.717μM
FRK(PTK5)	IC50: 1.884μM
CSK	IC50: 2.339μM
Src	IC50: 2.389μM

Solubility *

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.

Preparing Stock Solutions

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.