Anticancer agent 53

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Anticancer agent 53 

Anticancer agent 53 是一种强效抗癌剂。 Anticancer agent 53 显示出体外细胞毒性。Anticancer agent 53 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 S/G2/M 期。Anticancer agent 53 具有抗肿瘤活性且无明显毒性。

Anticancer agent 53

Anticancer agent 53 Chemical Structure

CAS No. : 1926985-18-3

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生物活性

Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity[1].

体外研究
(In Vitro)

Anticancer agent 53 (compound c20) (0-1000 nM; 72 h) shows cytotoxicity with IC50s of 2.3, 42.0, 4.3, 96.3, 24.0, 47.4 nM for Hep3B, MCF7, A549, MDA-MB-231, KB, KB-vin cells, respectively[1].
Anticancer agent 53 (0.025, 0.05, 0.1 µM; 48 h) induces apoptosis and cell cycle arrest in S/G2/M phases[1].
Anticancer agent 53 (0.1. 0.2 µM; 6 h) inhibits topoisomerase I activity in A549 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 0.025, 0.05, 0.1 µM
Incubation Time: 0-48 h
Result: Induced cell cycle arrest in S/G2/M phases.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 0.025, 0.05, 0.1 µM
Incubation Time: 0-48 h
Result: Induced apoptosis with the proapoptotic protein Caspase-3 and Bax were up-regulated and anti-apoptotic Bcl-2 was down-regulated.

体内研究
(In Vivo)

Anticancer agent 53 (5, 25 and 50 mg/kg; IP) shows no apparent toxicity to mouse liver, kidney and hemopoietic system[1].
Anticancer agent 53 (2 mg/kg; i.v; every other day for two weeks) shows antitumor effect in HCC mouse model[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/C mice[1]
Dosage: 5, 25 and 50 mg/kg (saline with 5% DMSO and 5% Cremophor EL)
Administration: I.p.
Result: Showed no body weight loss, no significant liver damage, no significant damage occurred in spleens and livers.
Animal Model: 6-8 weeks Female BALB/c nude mice (Hep3B cells)[1]
Dosage: 1, 2 mg/kg
Administration: I.v., every other day for total 7 doses
Result: Significantly inhibited tumor growth with an average body weight of 24 g and an average tumor volume of 3800 mm[3] at 1 mg/kg and an average body weight of 22 g and average tumor volume 2380 mm[3] at 2 mg/kg.
Animal Model: 6-8 weeks FVB/N mice (HCC mouse model)[1]
Dosage: 2 mg/kg
Administration: I.v.; every other day for two weeks
Result: Inhibited the tumor growth and reduced the liver weights, and t inhibited proliferation of HCC tissues.

分子量

600.62

Formula

C31H25FN4O6S
CAS 号

1926985-18-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Yang CJ, et al. Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin. Eur J Med Chem. 2020 Feb 1;187:111971.

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