Exatecan
- CAS NO.:171335-80-1
- Empirical Formula: C24H22FN3O4
- Molecular Weight: 435.45
- MDL number: MFCD00926120
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 23:02:33
What is Exatecan?
Description
Exatecan is a hexacyclic chemical compound analogous to camptothecin and used as a payload in ADC research. Exatecan mesylate is used as an inhibitor of DNA topoisomerase I, which plays a key role in DNA replication, transcription, and recombination.
Definition
ChEBI: Exatecan is a pyranoindolizinoquinoline.
Biological Activity
Exatecan (DX-8951) is a DNA topoisomerase I (topoisomerase I) inhibitor with IC50 of 2.2 μM (0.975 μg/mL) for cancer research.
in vitro
Exatecan is a potent topoisomerase I inhibitor, with an IC 50 of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI 50 s 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 GI 50 s 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.
Properties of Exatecan
Boiling point: | 818.4±65.0 °C(Predicted) |
Density | 1.53±0.1 g/cm3(Predicted) |
storage temp. | Store at -20°C,protect from light |
solubility | Soluble in DMSO |
form | Solid |
pka | 11.19±0.40(Predicted) |
color | Off-white to gray |
Safety information for Exatecan
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H332:Acute toxicity,inhalation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Exatecan
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