Exatecan

CAS No. 171335-80-1

Exatecan( —— )

Catalog No. M32922 CAS No. 171335-80-1

Exatecan (DX-8951f) is a DNA topoisomerase I (TOP1) inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL).Exatecan has antitumor activity and may be used in cancer research.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
10MG 29 Get Quote
25MG 59 Get Quote
50MG 86 Get Quote
100MG 124 Get Quote
500MG 305 Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    Exatecan
  • Note
    Research use only, not for human use.
  • Brief Description
    Exatecan (DX-8951f) is a DNA topoisomerase I (TOP1) inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL).Exatecan has antitumor activity and may be used in cancer research.
  • Description
    Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
  • In Vitro
    Exatecan is a potent topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI50s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells and lung cancer cells, respectively. Exatecan Mesylate (DX-8951f) displays cytotoxic activities against PC-6, PC-6/SN2-5 cells, with mean GI50s of 0.186 and 0.395 ng/mL, respctively. Exatecan Mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells.
  • In Vivo
    Exatecan Mesylate (DX-8951f, 3.325-50 mg/kg, i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death. Exatecan Mesylate (15, 25 mg/kg, i.v.) hightly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan Mesylate (15, 25 mg/kg, i.v.) also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model.
  • Synonyms
    ——
  • Pathway
    Antibody Drug Conjugates (ADC)
  • Target
    ADC Cytotoxin
  • Recptor
    ADC Cytotoxin | Topoisomerase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    171335-80-1
  • Formula Weight
    435.45
  • Molecular Formula
    C24H22FN3O4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 20 mg/mL (45.93 mM; Ultrasonic )
  • SMILES
    N[C@@H]1C2=C3C(C=4N(C3)C(=O)C5=C(C4)[C@](CC)(O)C(=O)OC5)=NC=6C2=C(CC1)C(C)=C(F)C6
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Mitsui I, et al. A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo. Jpn J Cancer Res. 1995 Aug;86(8):776-82.?
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