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IHMT-RAF-128

Chemical Structure : IHMT-RAF-128

CAS No.: 2479289-15-9

IHMT-RAF-128

Catalog No.: PC-20793Not For Human Use, Lab Use Only.

IHMT-RAF-128 is a highly potent pan-RAF inhibitor with IC50 of 5.9 and 3.6 nM for BRAF-V600E and CRAF, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

IHMT-RAF-128 is a highly potent pan-RAF inhibitor with IC50 of 5.9 and 3.6 nM for BRAF-V600E and CRAF, respectively.
IHMT-RAF-128 exhibits similarly high efficacies in inhibiting both partners of the RAF dimer.
IHMT-RAF-128 shows potent anti-tumor efficacy against a variety of cancer cells harboring either RAF or RAS mutations, especially Adagrasib and Sotorasib (AMG510) resistant-KRAS-G12C secondary mutations, such as KRAS-G12C-Y96C and KRAS-G12C-H95Q.
IHMT-RAF-128 shows excellent pharmacokinetic profile (PK), and the bioavailability in mice and rats were 63.9%, and 144.1%, respectively.
IHMT-RAF-128 exhibits potent anti-tumor efficacy on xenograft mouse tumor models in a dose-dependent manner without any obvious toxicities.

Physicochemical Properties

M.Wt 507.52
Formula C27H24F3N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(NC1=CC=C(C)C(N2N=CC(C3=CC(N4CCOCC4)=CN=C3)=C2)=C1)C5=CC=CC(C(F)(F)F)=C5

References

1. Aoli Wang, et al. Eur J Pharmacol. 2023 May 8;175752.

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