PF-3758309

For research use only. Not for therapeutic Use.

  • CAT Number: I005375
  • CAS Number: 898044-15-0
  • Molecular Formula: C25H30N8OS
  • Molecular Weight: 490.60
  • Purity: ≥95%
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PF-3758309(Cat No.:I005375)is a potent small-molecule inhibitor of PAK4 (p21-activated kinase 4), a serine/threonine kinase involved in regulating cell motility, survival, and proliferation. By inhibiting PAK4, PF-3758309 disrupts critical signaling pathways, including the MAPK and PI3K/Akt pathways, which are often dysregulated in cancer. This compound has shown promise in preclinical studies for its ability to halt tumor growth and induce apoptosis in cancer cells. PF-3758309 is widely used in cancer research to explore the therapeutic potential of targeting PAK4 in various cancers, including pancreatic and breast cancer.


Catalog Number I005375
CAS Number 898044-15-0
Synonyms

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

Molecular Formula C25H30N8OS
Purity ≥95%
Target PAK4
Solubility 10 mM in DMSO
Storage Store at -20°C
IC50 1.3 nM (PAK4)
IUPAC 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
InChI InChI=1S/C25H30N8OS/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)/t19-/m1/s1
InChIKey AYCPARAPKDAOEN-LJQANCHMSA-N
SMILES CC1=NC2=C(C(=N1)NC3=NNC4=C3CN(C4(C)C)C(=O)N[C@H](CN(C)C)C5=CC=CC=C5)SC=C2
Reference

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<br>[1]. Murray, Brion W.; Guo, Chuangxing; Piraino, Joseph. Small-molecule p21-activated kinase inhibitor PF3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proceedings of the National Academy of Sciences of the United States of America (2010), 107(20), 9446-9451, S9446/1-S9446/18.
<br>[2]. Murray BW, Guo C, Piraino J, Westwick JK, Zhang C, Lamerdin J, Dagostino E, Knighton D, Loi CM, Zager M, Kraynov E, Popoff I, Christensen JG, Martinez R, Kephart SE, Marakovits J, Karlicek S, Bergqvist S, Smeal T. Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc Natl Acad Sci U S A. 2010 May 18;107(20):9446-51.
<br>[3]. Zhao ZS, Manser E. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70.
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