Description
PF-3758309 dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
Product information
Molecular Weight: 563.55
Formula: C25H32Cl2N8OS
Chemical Name: N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6, 6-dimethyl-3-[(2-methylthieno[3, 2-d]pyrimidin-4-yl)amino]-1, 4-dihydropyrrolo[3, 4-c]pyrazole-5-carboxamide;dihydrochloride
Smiles: Cl.Cl.CN(C)C[C@@H](NC(=O)N1CC2C(NC3=NC(C)=NC4C=CSC=43)=NNC=2C1(C)C)C1C=CC=CC=1
InChiKey: BTVSNRMSUYBDRT-JQDLGSOUSA-N
InChi: InChI=1S/C25H30N8OS.2ClH/c1-15-26-18-11-12-35-20(18)23(27-15)29-22-17-13-33(25(2,3)21(17)30-31-22)24(34)28-19(14-32(4)5)16-9-7-6-8-10-16;;/h6-12,19H,13-14H2,1-5H3,(H,28,34)(H2,26,27,29,30,31);2*1H/t19-;;/m1../s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
PF-3758309 dihydrochloride has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC50=190 nM; PAK3, IC50=99 nM). In cells, PF-3758309 dihydrochloride inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50=4.7 nM). PF-3758309 dihydrochloride also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC50=20 nM) and anchorage-independent growth (IC50=27 nM) of A549 cells.
In Vivo:
PF-3758309 dihydrochloride (7.5-30 mg/kg; p.o.; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models.
Products are for research use only. Not for human use.
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