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HIT220912755
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HIT220912755
  • HIT ID:HIT220912755
  • Cas No:1202401-59-9
  • 常用名:PC-046
  • IUPAC:3-(3-methoxyphenyl)-4-[5-(4-methoxyphenyl)-1,3-oxazol-2-yl]pyridine
    IUPAC:3-(3-methoxyphenyl)-4-[5-(4-methoxyphenyl)-1,3-oxazol-2-yl]pyridine
  • InChI key:InChIKey=CTNUOHRUVZXVHX-UHFFFAOYSA-N
  • 分子式:C22H18N2O3
  • 分子量:358.397
  • 氢键供体数 (HBD):
  • 氢键受体数 (HBA):
  • LogP:
  • SMILES:COc1ccc(cc1)-c1cnc(o1)-c1ccncc1-c1cccc(OC)c1
    SMILES:COc1ccc(cc1)-c1cnc(o1)-c1ccncc1-c1cccc(OC)c1
  • 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......
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  • 供应商
    TargetMolSC
    规格
    货期
    6-8周
    纯度
    -
    ¥ 10,600.00
    1

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