Belotecan

Modify Date: 2024-01-02 12:04:13

Belotecan Structure
Belotecan structure
Common Name Belotecan
CAS Number 256411-32-2 Molecular Weight 433.500
Density 1.4±0.1 g/cm3 Boiling Point 772.4±60.0 °C at 760 mmHg
Molecular Formula C25H27N3O4 Melting Point N/A
MSDS N/A Flash Point 420.9±32.9 °C

 Use of Belotecan


Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer[1].

 Names

Name Camtobell
Synonym More Synonyms

 Belotecan Biological Activity

Description Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer[1].
Related Catalog
Target

IC50: 30 ng/mL (Caski cells), 150 ng/mL (HeLa cells), 150 ng/mL (SiHa cells)[1]

In Vitro Belotecan (0-600 ng/mL; 0-72 h) time- and dose-dependently inhibits viability of Caski cells, HeLa cells and SiHa cells at 48 h with IC50 values of 30, 150 and 150 ng/mL, respectively[1]. Belotecan (0-150 ng/mL; 48 h) induces cell apoptosis and cell-cycle arrest, and affects PARP, cleaved PARP, BAX, p53, Ser15, cell cycle related protein expression and cancer invasion in cervical cancer[1]. Apoptosis Analysis[1] Cell Line: Caski, HeLa and SiHa cell lines Concentration: 0-150 ng/mL Incubation Time: 48 h Result: Showed strong pro-apoptotic activities to Caski, HeLa and SiHa cells. Western Blot Analysis[1] Cell Line: Caski, HeLa and SiHa cell lines Concentration: 0-150 ng/mL Incubation Time: 48 h Result: Increased the expression of PARP, cleaved PARP, BAX, p53, Ser15, cyclin B1, phosphorylated cyclin B1 and phospho-cdc2 (Tyr15) protein, and decreased MMP2 and VEGF protein expression. Cell Cycle Analysis[1] Cell Line: Caski, HeLa and SiHa cell lines Concentration: 0-150 ng/mL Incubation Time: 48 h Result: Induced cell-cycle arrest in the G2/M phase in cervical cancer. Cell Invasion Assay[1] Cell Line: Caski, HeLa and SiHa cell lines Concentration: 0-150 ng/mL Incubation Time: 48 h Result: Inhibited cancer invasion in cervical cancer.
In Vivo Belotecan (25 mg/kg; i.v. for 16 days at 4-day intervals) inhibits tumor growth in CaSki-xenografts nude mice[1]. Animal Model: BALB/c-nude mice with CaSki cells injection[1] Dosage: 25 mg/kg Administration: Intravenous injection; 25 mg/kg; 16 days at 4-day intervals Result: Significantly inhibited the tumor growth and showed no significant difference in bodyweight of xenograft mice and the controls.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 772.4±60.0 °C at 760 mmHg
Molecular Formula C25H27N3O4
Molecular Weight 433.500
Flash Point 420.9±32.9 °C
Exact Mass 433.200165
PSA 93.45000
LogP 1.86
Vapour Pressure 0.0±2.8 mmHg at 25°C
Index of Refraction 1.679

 Synonyms

Belotecan
7-(2-(N-Isopropylamino)ethyl)camptothecin
(4S)-4-Ethyl-4-hydroxy-11-[2-(isopropylamino)ethyl]-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
Belotecan [INN]
CKD602
UNII-27Z82M2G1N
(4S)-4-Ethyl-4-hydroxy-11-(2-(isopropylamino)ethyl)-1,12-dihydro-14H-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4H)-dione
1H-Pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, 4-ethyl-4-hydroxy-11-[2-[(1-methylethyl)amino]ethyl]-, (4S)-
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