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$0.00 - 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
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 |
|---|---|
| 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 |
| 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 |
| 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. |
Datasheet
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