MedKoo Cat#: 121073 | Name: Exarafenib
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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
Exarafenib
CAS#2639957-39-2 (free base)

Theoretical Analysis

MedKoo Cat#: 121073

Name: Exarafenib

CAS#: 2639957-39-2 (free base)

Chemical Formula: C26H34F3N5O3

Exact Mass: 521.2614

Molecular Weight: 521.59

Elemental Analysis: C, 59.87; H, 6.57; F, 10.93; N, 13.43; O, 9.20

Price and Availability

Size Price Availability Quantity
5mg USD 450.00 2 Weeks
10mg USD 800.00 2 Weeks
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Synonym
Exarafenib, RAF/KIN_2787; KIN-2787; KIN 2787; KIN2787;
IUPAC/Chemical Name
(3S)-N-{3-[2-{[(2R)-1-hydroxypropan-2-yl]amino}-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl}-3-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide
InChi Key
GZMYLSJUNSCMTD-MOPGFXCFSA-N
InChi Code
InChI=1S/C26H34F3N5O3/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)/t18-,19+/m1/s1
SMILES Code
O=C(N1CC[C@@H](CC(F)(F)F)C1)NC2=CC(C3=CC(N[C@H](C)CO)=NC(N4CCOCC4)=C3)=C(C)C=C2
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

Preparing Stock Solutions

The following data is based on the product molecular weight 521.59 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL