Free shipping on all orders over $ 500

Belvarafenib (GDC5573, HM95573, RG6185)

Cat. No. M20678
Belvarafenib (GDC5573, HM95573, RG6185) Structure
Size Price Availability
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Belvarafenib (GDC5573, HM95573, RG6185) is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively.

Chemical Information
Molecular Weight 478.93
Formula C23H16ClFN6OS
CAS Number 1446113-23-0
Solubility (25°C) DMSO 96 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Yu-Yon Kim, et al. Clin Exp Metastasis. Belvarafenib penetrates the BBB and shows potent antitumor activity in a murine melanoma brain metastasis model

[2] Gil Awada, et al. Curr Opin Oncol. Melanoma with genetic alterations beyond the BRAFV600 mutation: management and new insights

[3] Robert Roskoski Jr. Pharmacol Res. Blockade of mutant RAS oncogenic signaling with a special emphasis on KRAS

[4] No authors listed. Cancer Discov. ARAF Mutations Limit Response to RAF Dimer Inhibition

[5] Ivana Yen, et al. Nature. ARAF mutations confer resistance to the RAF inhibitor belvarafenib in melanoma

Related Raf Products
Cyclorasin 9A5

Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM.

R18

R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM.

PROTAC RAF degrader 1

PROTAC RAF degrader 1 is a PROTAC RAF degrader.

B-Raf IN 15

B-Raf IN 15 is a BRAF inhibitor.

Raf inhibitor 3

Raf inhibitor 3 is a Raf inhibitor.

  Catalog
Abmole Inhibitor Catalog




Keywords: Belvarafenib (GDC5573, HM95573, RG6185) supplier, Raf, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.