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HomeProduct name listExatecan

Exatecan

Exatecan Structural

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)
ghs
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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