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GFH375

Chemical Structure : GFH375

CAS No.:

GFH375 (VS-7375, GFH-375, VS7375)

Catalog No.: PC-28259Not For Human Use, Lab Use Only.

GFH375 (VS-7375) is an orally bioavailable, noncovalent, selective KRAS G12D inhibitor, targets both 'ON' (GTP-bound) and 'OFF' (GDP-bound) states of KRASG12D proteins.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GFH375 (VS-7375) is an orally bioavailable, noncovalent, selective KRAS G12D inhibitor, targets both 'ON' (GTP-bound) and 'OFF' (GDP-bound) states of KRASG12D proteins.
GFH375 demonstrates potent signaling pathway inhibition and antitumor activity in preclinical KRASG12D-driven tumor models, with minimal off-target effects.

Physicochemical Properties

M.Wt 656.73
Formula C36H31D3F3N7O2
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

4-((5S,6S,9R)-12-(((S)-2-(difluoromethylene)tetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-1-fluoro-5-(methyl-d3)-5a,6,7,8,9,10-hexahydro-5H-4-oxa-3,10a,11,13,14-pentaaza-6,9-methanonaphtho[1,8-ab]heptalen-2-yl)-5-ethynylnaphthalen-2-amine

References

1. Ai X, et al. Nat Med. 2026 Sep;32(9):3302-3312.

2. Yan, F. et al. GFH375 (VS-7375): an oral, selective KRAS G12D (ON/OFF) inhibitor with potent anti-tumor efficacy. Cancer Res. 84, abstr.3318 (2024).

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