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RAF-709

CAS No. 1628838-42-5

RAF-709( RAF709 | RAF 709 )

Catalog No. M12436 CAS No. 1628838-42-5

A novel potent, selective, and orally bioavailable RAF inhibitor with biochemical IC50 of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    RAF-709
  • Note
    Research use only, not for human use.
  • Brief Description
    A novel potent, selective, and orally bioavailable RAF inhibitor with biochemical IC50 of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively.
  • Description
    A novel potent, selective, and orally bioavailable RAF inhibitor with biochemical IC50 of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively; suppresses pERK (EC50=0.02-0.1 uM), stabilizes BRAF CRAF dimers(EC50=0.8 uM) inhibits proliferation (EC50=0.95 uM) in KRAS mutant tumor cell lines (Calu6); shows effectivity in a KRAS mutant xenograft model.
  • In Vitro
    RAF709 stabilizes BRAF-CRAF dimers with an EC50 of 0.8 μM. In cellular assays, the dose-response of pMEK and pERK are measured in Calu-6 cells with EC50=0.02 and 0.1 μM with minimal paradoxical activation and inhibition of proliferation with EC50=0.95 μM.
  • In Vivo
    RAF709 proves to be soluble, kinase selective, and efficacious in a KRAS mutant xenograft model. RAF709 shows dose-proportional increases in plasma exposure and a corresponding dosedependent inhibition of pERK in Calu-6 tumors. Treatment with RAF709 results in dose-dependent antitumor activity with 10 mg/kg being subefficacious (%T/C=92%), 30 mg/kg results in measurable antitumor activity (%T/C=46%), and 200 mg/kg results in mean tumor regression of 92%, while the same high dose is not efficacious in the PC3, KRAS WT model.
  • Synonyms
    RAF709 | RAF 709
  • Pathway
    MAPK/ERK Signaling
  • Target
    Raf
  • Recptor
    B-Raf|C-Raf
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1628838-42-5
  • Formula Weight
    542.5495
  • Molecular Formula
    C28H29F3N4O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 100 mg/mL
  • SMILES
    CC1=C(C=C(C=N1)NC(=O)C2=CC(=CC=C2)C(F)(F)F)C3=CC(=C(N=C3)OC4CCOCC4)N5CCOCC5
  • Chemical Name
    Benzamide, N-[2-methyl-5'-(4-morpholinyl)-6'-[(tetrahydro-2H-pyran-4-yl)oxy][3,3'-bipyridin]-5-yl]-3-(trifluoromethyl)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Nishiguchi GA, et al. J Med Chem. 2017 Jun 22;60(12):4869-4881.
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