Gimatecan

CAS No. 292618-32-7

Gimatecan( —— )

Catalog No. M33718 CAS No. 292618-32-7

Gimatecan (STI481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 176 Get Quote
5MG 274 Get Quote
10MG 454 Get Quote
25MG 726 Get Quote
50MG 994 Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    Gimatecan
  • Note
    Research use only, not for human use.
  • Brief Description
    Gimatecan (STI481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
  • Description
    Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
  • In Vitro
    Gimatecan (3 to 300 ng/mL) significantly inhibits the growth of human bladder cancer models (HT1376 and MCR), thus reflecting antiproliferative potency.Gimatecan causes a persistent S-phase arrest At 0.003 μg/mL and the number of S-phase cells increased after treatment with a higher concentration (0.03 μg/mL).Cell Proliferation AssayCell Line:HT1376 cells harbor a p53 mutation; MCR cells harbor two p53 mutations: one in exon 4 (CGC→CCC) and one in exon 9 (CAG→TAG)Concentration:3 to 300 ng/mL Incubation Time:1, 6, and 24 hours Result:IC50s of 90±3 and 9.0±0.4 ng/mL for MCR and HT1376 cells after treatment for 1 hours. IC50s of 5.0±0.2 and 2.8±0.1 ng/mL for MCR and HT1376 cells after treatment for 24 hours. The growth-inhibitory effect was dose-dependent and time-dependent. HT1376 cells were more sensitive than MCR cells at least following a short-term exposure.
  • In Vivo
    Gimatecan (2 mg/kg; treatment per os, every fourth day for four times) is effective for inhibiting tumor growth.Animal Model:Athymic Swiss nude mice bearing HT1376 model Dosage:2 mg/kg Administration:Treatment per os, every fourth day for four times Result:Caused a marked tumor growth inhibition during treatment.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    Topoisomerase
  • Recptor
    Topoisomerase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    292618-32-7
  • Formula Weight
    447.48
  • Molecular Formula
    C25H25N3O5
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 33.33 mg/mL (74.48 mM; ultrasonic and warming and adjust pH to 10 with NaOH and heat to 60°C; )
  • SMILES
    CC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4ccccc4c(\C=N\OC(C)(C)C)c3Cn1c2=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Paola Ulivi, et al. Cellular Basis of Antiproliferative and Antitumor Activity of the Novel Camptothecin Derivative, Gimatecan, in Bladder Carcinoma Models. Neoplasia. 2005 Feb;7(2):152-61.?
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