Padnarsertib

Last updated

Padnarsertib
Padnarsertib structure.png
Clinical data
Drug class NAMPT / PAK4 dual inhibitor
Identifiers
  • (E)-3-(6-amino-3-pyridinyl)-N-[[5-[4-(4,4-difluoropiperidine-1-carbonyl)phenyl]-7-(4-fluorophenyl)-1-benzofuran-2-yl]methyl]prop-2-enamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C35H29F3N4O3
Molar mass 610.637 g·mol−1
3D model (JSmol)
  • C1CN(CCC1(F)F)C(=O)C2=CC=C(C=C2)C3=CC(=C4C(=C3)C=C(O4)CNC(=O)/C=C/C5=CN=C(C=C5)N)C6=CC=C(C=C6)F
  • InChI=1S/C35H29F3N4O3/c36-28-9-7-24(8-10-28)30-19-26(23-3-5-25(6-4-23)34(44)42-15-13-35(37,38)14-16-42)17-27-18-29(45-33(27)30)21-41-32(43)12-2-22-1-11-31(39)40-20-22/h1-12,17-20H,13-16,21H2,(H2,39,40)(H,41,43)/b12-2+
  • Key:MRFOPLWJZULAQD-SWGQDTFXSA-N

Padnarsertib (KPT-9274), is a drug which acts as a dual inhibitor of the enzymes p21-activated kinase 4 (PAK4) and nicotinamide phosphoribosyltransferase (NAMPT). It has potential applications in the treatment of some forms of cancer. [1] [2] [3] [4] [5] [6] [7]

References

  1. ↑ Abu Aboud O, Chen CH, Senapedis W, Baloglu E, Argueta C, Weiss RH (September 2016). "Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth". Molecular Cancer Therapeutics. 15 (9): 2119–2129. doi:10.1158/1535-7163.MCT-16-0197. PMC   5010932 . PMID   27390344.
  2. ↑ Takao S, Chien W, Madan V, Lin DC, Ding LW, Sun QY, et al. (March 2018). "Targeting the vulnerability to NAD+ depletion in B-cell acute lymphoblastic leukemia". Leukemia. 32 (3): 616–625. doi:10.1038/leu.2017.281. PMID   28904384.
  3. ↑ Mpilla G, Aboukameel A, Muqbil I, Kim S, Beydoun R, Philip PA, et al. (November 2019). "PAK4-NAMPT Dual Inhibition as a Novel Strategy for Therapy Resistant Pancreatic Neuroendocrine Tumors". Cancers. 11 (12): 1902. doi: 10.3390/cancers11121902 . PMC   6966587 . PMID   31795447.
  4. ↑ Cordover E, Wei J, Patel C, Shan NL, Gionco J, Sargsyan D, et al. (February 2020). "KPT-9274, an Inhibitor of PAK4 and NAMPT, Leads to Downregulation of mTORC2 in Triple Negative Breast Cancer Cells". Chemical Research in Toxicology. 33 (2): 482–491. doi:10.1021/acs.chemrestox.9b00376. PMC   9316853 . PMID   31876149.
  5. ↑ Li Y, Lu Q, Xie C, Yu Y, Zhang A (2022). "Recent advances on development of p21-activated kinase 4 inhibitors as anti-tumor agents". Frontiers in Pharmacology. 13 956220. doi: 10.3389/fphar.2022.956220 . PMC   9465411 . PMID   36105226.
  6. ↑ Mogol AN, Kaminsky AZ, Dutton DJ, Madak Erdogan Z (March 2024). "Targeting NAD+ Metabolism: Preclinical Insights into Potential Cancer Therapy Strategies". Endocrinology. 165 (5) bqae043. doi:10.1210/endocr/bqae043. PMID   38565429.
  7. ↑ Wang Y, Minden A (September 2024). "Inhibition of NAMPT by PAK4 Inhibitors". International Journal of Molecular Sciences. 25 (18) 10138. doi: 10.3390/ijms251810138 . PMC   11431865 . PMID   39337621.
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