Anticancer agent 53

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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.

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Anticancer agent 53 Chemical Structure

CAS No. : 1926985-18-3

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	4.3 nM Compound: c20	Cytotoxicity against human A549 cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 31881457]
Hep 3B2	IC₅₀	2.3 nM Compound: c20	Cytotoxicity against human Hep3B cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human Hep3B cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 31881457]
KB	IC₅₀	24 nM Compound: c20	Cytotoxicity against human KB cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human KB cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 31881457]
MCF7	IC₅₀	42 nM Compound: c20	Cytotoxicity against human MCF7 cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 31881457]
MDA-MB-231	IC₅₀	96.3 nM Compound: c20	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 31881457]

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].

MedChemExpress (MCE) 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.

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].

MedChemExpress (MCE) 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.

Molecular Weight

600.62

Formula

C₃₁H₂₅FN₄O₆S

CAS No.

1926985-18-3

SMILES

CC[C@]1(C(OCC2=C1C=C3C4=NC5=CC=CC=C5C=C4CN3C2=O)=O)OC([C@@H](NC(NC(C6=CC=C(C=C6)F)=O)=S)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]