WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406313
Description: 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 studies show that PC-046 is a synthetically-derived, small molecule microtubule destabilizing agent. Advantages over existing microtubule destabilizing agents include ease of synthesis, lack of MDR cross-resistance, good oral bioavailability and the lack of acute myelotoxicity. (source: Invest New Drugs. 2013 Dec;31(6):1616-25. ).
MedKoo Cat#: 406313
Chemical Formula: C22H18N2O3
Exact Mass: 358.13
Molecular Weight: 358.38992
Elemental Analysis: C, 73.73; H, 5.06; N, 7.82; O, 13.39
Synonym: FTI2153; FTI 2153; FTI2153
IUPAC/Chemical Name: 5-(4-methoxyphenyl)-2-(3-(3-methoxyphenyl)pyridin-4-yl)oxazole
InChi Key: CTNUOHRUVZXVHX-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H18N2O3/c1-25-17-8-6-15(7-9-17)21-14-24-22(27-21)19-10-11-23-13-20(19)16-4-3-5-18(12-16)26-2/h3-14H,1-2H3
SMILES Code: COC1=CC(C2=C(C3=NC=C(C4=CC=C(OC)C=C4)O3)C=CN=C2)=CC=C1
1: Landowski TH, Samulitis BK, Dorr RT. The diaryl oxazole PC-046 is a tubulin-binding agent with experimental anti-tumor efficacy in hematologic cancers. Invest New Drugs. 2013 Dec;31(6):1616-25. doi: 10.1007/s10637-013-0019-8. Epub 2013 Sep 14. PubMed PMID: 24037082.