PC-046 - CAS 1202401-59-9

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine) . Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

Others, IRAK, Apoptosis, Pim, Trk receptor

Tyrosine Kinase/Adaptors, Apoptosis, JAK/STAT signaling, NF-κB, Immunology/Inflammation, Others, Chromatin/Epigenetic

1202333

C22H18N2O3

358.39

O(C)C=1C=C(C=2C(=CC=NC2)C=3OC(=CN3)C4=CC=C(OC)C=C4)C=CC1

-20°C

Ice Packs

Small Compound