KPT-9274
KPT-9274 is a potent, specific, dual NAMPT and PAK4 inhibitor with IC50 of 120 nM (NAMPT), also is an orally bioavailable PAK4 allosteric modulator with IC50 of 30 nM in MS-751 cell MTT assay; attenuates the PAK4/β-catenin pathway, results in NAD depletion, and attenuates viability, invasion, and migration in several RCC cell lines (IC50=600 nM for Caki-1 cells) ; attenuates G2/M transit and induces apoptosis, shows specificity for attenuation of NAD biosynthesis targets preferentially in RCC cells; decreases tumor growth in xenograft model of RCC.Blood Cancer Phase 1 Clinical.
Product Specifications
CAS Number
1643913-93-2
Product Name Alternative
KPT9274
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 32 mg/mL
Smiles
OC (/C=C/C1=NC (N) =CC=C1) =N\CC2=CC3=CC (C4=CC=C (C (N5CCC (F) (F) CC5) =O) C=C4) =CC (C6=CC=C (F) C=C6) =C3O2
Molecular Formula
C35H29F3N4O3
Molecular Weight
610.625
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2-Propenamide, 3- (6-amino-3-pyridinyl) -N-[[5-[4-[ (4,4-difluoro-1-piperidinyl) carbonyl]phenyl]-7- (4-fluorophenyl) -2-benzofuranyl]methyl]-, (2E) -
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