918504-65-1
Vemurafenib
CAS: 1029872-54-5;918504-65-1
Molecular Formula: C23H18ClF2N3O3S
918504-65-1 - Names and Identifiers
918504-65-1 - Physico-chemical Properties
| Molecular Formula | C23H18ClF2N3O3S |
| Molar Mass | 489.9221264 |
| Density | 1.46 |
| Melting Point | >263oC (dec.) |
| Solubility | Soluble in DMSO (100 mg/mL), and methanol. Insoluble in ethanol, and water |
| Appearance | Solid |
| Color | Off-White |
| Storage Condition | Refrigerator |
| Use | A novel and potent inhibitor of B- RAFV600E with IC50 of 31 nM. |
918504-65-1 - Reference
| Reference Show more | 1. [IF=9.162] Kun Zhao et al."Morusin enhances the antitumor activity of MAPK pathway inhibitors in BRAF-mutant melanoma by inhibiting the feedback activation of STAT3."Eur J Cancer. 2022 Apr;165:58 |
918504-65-1 - Introduction
Vemurafenib (PLX4032, RG7204) is a new and effective B- Raf V600E inhibitor with IC50 of 31 nM.
Last Update：2022-10-16 17:11:36
918504-65-1 - Reference Information
| overview | vilafenib (Vemurafenib), trade name Zelboraf, is a kinase inhibitor developed by Roche (HoffmannLaRoche) company for the treatment of patients with unresectable or metastatic melanoma and BRAFV600E mutations approved by FDA. it was approved by FDA in August 2011 for the treatment of advanced metastatic or unresectable melanoma. |
| Application | Verofenib is a small molecule BRAF kinase inhibitor that can selectively bind to the ATP binding domain of mutant BRAF, thereby inhibiting the activation of the enzyme. The US Food and Drug Administration (FDA) has approved Verofenib for the treatment of malignant melanoma with BRAF gene mutation. |
| preparation | preparation of vilafenib (I): add 250g of toluene and 31.5g (0.10 mol) N-[2] to a 500 ml four-mouth flask connected with stirring, thermometer and reflux condenser tube with water separator, 4-Difluoro-3-(cyanopropionyl) phenyl] n-propyl sulfonamide, 17.0 grams (0.11 moles) of p-chlorophenyl acetaldehyde, 0.5 grams of piperidine, heating, stirring, 83-85 ℃ azeotropic reflux with water Condensation reaction for 5 hours; cooling to 30 ℃, adding 38.0 grams (0.32 moles) of N,N-dimethylformamide dimethanol, stirring at 85-90 ℃ for 6 hours; cooling to 30 ℃, 70.0g of 10wt% ammonia methanol solution was added and stirred at 50~55 ℃ for 4 hours. Decompression distillation recovers methanol and toluene, adds 200 grams of isopropanol to the residue, heats to 80 ℃, cools, recrystallizes, filters, dries to obtain 43.9 kverafenib with 89.6% yield and 99.91% liquid phase purity. |
Last Update：2024-04-09 21:11:58
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Product Name: Vemurafenib Visit Supplier Webpage Request for quotationCAS: 918504-65-1
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: Vemurafenib (PLX4032, RG7204) Visit Supplier Webpage Request for quotationCAS: 918504-65-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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