Exatecan

SKU: orb1709722

Description

Exatecan (DX-8951f) is a DNA topoisomerase I inhibitor with an IC50 of 2.2 μM, demonstrating antitumor activity. It is used in cancer research for in vitro cell line assays and in vivo animal models, as reported in preclinical studies on topoisomerase-targeted therapies.

Research Area

Molecular Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 171335-80-1
• MW: 435.45
• Purity: 99.64% (May vary between batches)
• Formula: C₂₄H₂₂FN₃O₄
• 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
• Target: Topoisomerase,ADC Cytotoxin
• Solubility: DMSO:20 mg/mL (45.93 mM)

Bioactivity

• Target IC50:
  Topo I:2.2 μM
• In Vivo:
  Exatecan (DX-8951f) (3.325-50 mg/kg; i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death. Exatecan (15, 25 mg/kg; i.v.) highly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model.
  Read more...
• In Vitro:
  Exatecan (DX-8951f) displays cytotoxic activities against PC-6, and PC-6/SN2-5 cells, with mean GI50s of 0.186 and 0.395 ng/mL, respectively. Exatecan (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells. Exatecan is a potent topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL. Exatecan 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.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ADCCytotoxin, ADC Cytotoxin, DX8951, DX-8951f, DX 8951, Exatecan, Topoisomerase I, topoisomerase I

Compound Identifiers

PubChem CID

151115