Exarafenib HCl | CAS#2639957-39-2 |RAF inhibitor| MedKoo

MedKoo Cat#: 124446 | Name: Exarafenib HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Exarafenib, also known as KIN-2787, is a potent, selective pan-RAF inhibitor with activity in preclinical models of BRAF class II/III mutant and NRAS mutant melanoma. Exarafenib demonstrated exceptional kinome selectivity with minimal off-target kinases significantly inhibited relative to BRAF. Exarafenib potently inhibited a broad panel of oncogenic BRAF mutations in biochemical and BaF3 cell assays. Functional MAPK signaling and viability studies in human tumor cell lines highlighted exarafenib activity in BRAF and NRAS mutant melanoma with minimal activity in normal (BRAF WT) cells.

Chemical Structure

Exarafenib HCl

CAS#Exarafenib HCl

Theoretical Analysis

MedKoo Cat#: 124446

Name: Exarafenib HCl

CAS#: Exarafenib HCl

Chemical Formula: C26H35ClF3N5O3

Exact Mass: 557.2400

Molecular Weight: 558.04

Elemental Analysis: C, 55.96; H, 6.32; Cl, 6.35; F, 10.21; N, 12.55; O, 8.60

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

Exarafenib HCl 2639957-39-2 (free base)

Synonym

Exarafenib hydrochloride; RAF/KIN_2787; KIN-2787; KIN 2787; KIN2787;

IUPAC/Chemical Name

(3S)-N-[3-[2-[[(2R)-1-hydroxypropan-2-yl]amino]-6-morpholin-4-ylpyridin-4-yl]-4-methylphenyl]-3-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide;hydrochloride

InChi Key

DTAKPQLNXDAFGP-VOMIJIAVSA-N

InChi Code

InChI=1S/C26H34F3N5O3.ClH/c1-17-3-4-21(31-25(36)34-6-5-19(15-34)14-26(27,28)29)13-22(17)20-11-23(30-18(2)16-35)32-24(12-20)33-7-9-37-10-8-33;/h3-4,11-13,18-19,35H,5-10,14-16H2,1-2H3,(H,30,32)(H,31,36);1H/t18-,19+;/m1./s1

SMILES Code

O=C(N1C[C@H](CC(F)(F)F)CC1)NC2=CC=C(C)C(C3=CC(N[C@H](C)CO)=NC(N4CCOCC4)=C3)=C2.[H]Cl

Appearance

To be determined

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

MAPK activating mutations are common in melanoma, with 40% of cases attributed to oncogenic BRAF mutations and 20-25% NRAS mutations. Secondary MAPK activation is a known resistance mechanism to approved BRAF inhibitors in BRAFV600 melanoma. While BRAF inhibitors are approved for Class I BRAFV600 melanomas, patients with dimer-driven BRAF Class II/III and RAF1-dependent NRAS activated melanomas lack approved targeted therapy. Development of next-gen pan-RAF inhibitors targeting all RAF proteins and mutant dimers remains a priority. Emerging clinical data from pan-RAF inhibitors combined with MEK inhibitors suggests increased benefit for MAPK-altered melanoma patients

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 558.04 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.