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Exarafenib

Cat. No. M22476
Exarafenib Structure
Synonym:

KIN-2787

Size Price Availability Quantity
25mg USD 1350  USD1350 In stock
50mg USD 2200  USD2200 In stock
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Quality Control & Documentation
Biological Activity

Exarafenib (KIN-2787) is a highly selective, potent, next-generation, pan-RAF inhibitor with activity across BRAF and RAS mutant human tumor cell models. Exarafenib has anticancer activity by suppression of downstream MAPK pathway signaling. KIN-2787 in combination with binimetinib demonstrated significant combination benefit in NRAS mutant melanoma models.

Chemical Information
Molecular Weight 521.58
Formula C26H34F3N5O3
CAS Number 2639957-39-2
Solubility (25°C) DMSO 90 mg/mL
Storage 4°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Enrico Tiacci, et al. N Engl J Med. Vemurafenib plus Rituximab in Refractory or Relapsed Hairy-Cell Leukemia

[2] Ralf Gutzmer, et al. Lancet. Atezolizumab, vemurafenib, and cobimetinib as first-line treatment for unresectable advanced BRAFV600 mutation-positive melanoma (IMspire150): primary analysis of the randomised, double-blind, placebo-controlled, phase 3 trial

[3] Claus Garbe, et al. Recent Results Cancer Res. Vemurafenib

[4] Reinhard Dummer, et al. Lancet Oncol. Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial

[5] Claus Garbe, et al. Recent Results Cancer Res. Vemurafenib

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