PC-046

CAT: 0931-T71252-01Size: 25 mgDry Ice: NoHazardous: No
CAT#:0931-T71252-01Size:25 mg
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CAS Number
1202401-59-9
Target
Others|||IRAK|||Apoptosis|||Pim|||Trk receptor
Related Pathways
Tyrosine Kinase/Adaptors|||Apoptosis|||JAK/STAT signaling|||NF-?B|||Immunology/Inflammation|||Others|||Chromatin/Epigenetic
Bioactivity
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......
Smiles
O(C)C=1C=C(C=2C(=CC=NC2)C=3OC(=CN3)C4=CC=C(OC)C=C4)C=CC1
Molecular Formula
C22H18N2O3
Molecular Weight
358.39
Shipping Conditions
Cool pack
Storage Temperature
-20°C

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