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Cat. No.: HY-115996

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Antitumor agent-51

Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC₅₀ of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity.

For research use only. We do not sell to patients.

CAS No.: 3035774-65-0
Formula: C₂₃H₂₅N₅O₂S
Molecular Weight:435.54

Storage:

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

Data Sheet (274 KB)

Antitumor agent-51 Chemical Structure

CAS No.: 3035774-65-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC₅₀: 21.9 nM in MNNG/HOS cells^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
143B	IC₅₀	29.5 nM Compound: (R)-8i	Antiproliferative activity against human 143B cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human 143B cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 34861640]
GES1	IC₅₀	>20 μM Compound: (R)-8i	Cytotoxicity against human GES1 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay Cytotoxicity against human GES1 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 34861640]
HL-60	IC₅₀	19 nM Compound: (R)-8i	Antiproliferative activity against human HL-60 cells with low MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL-60 cells with low MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 34861640]
HOS	IC₅₀	50.88 nM Compound: (R)-8i	Antiproliferative activity against human HOS cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human HOS cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 34861640]
HOS-TE85	IC₅₀	0.022 μM Compound: R-8i	Antiproliferative activity against human MNNG/HOS cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MNNG/HOS cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38232462]
HOS-TE85	IC₅₀	21.9 nM Compound: (R)-8i	Antiproliferative activity against human MNNG/HOS cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human MNNG/HOS cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 34861640]
HOS-TE85	IC₅₀	31.6 nM Compound: (R)-8i	Antiproliferative activity against human MNNG/HOS cells with increase MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MNNG/HOS cells with increase MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 34861640]
HOS-TE85	IC₅₀	35.23 nM Compound: (R)-8i	Antiproliferative activity against human MNNG/HOS cells with low MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MNNG/HOS cells with low MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 34861640]
K562	IC₅₀	28.1 nM Compound: (R)-8i	Antiproliferative activity against human K562 cells with low MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells with low MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 34861640]
MG-63	IC₅₀	14.9 nM Compound: (R)-8i	Antiproliferative activity against human MG-63 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human MG-63 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 34861640]
MG-63	IC₅₀	14.9 nM Compound: (R)-8i	Antiproliferative activity against human MG-63 cells with increase MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MG-63 cells with increase MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 34861640]
SAOS-2	IC₅₀	26.8 nM Compound: (R)-8i	Antiproliferative activity against human SAOS-2 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human SAOS-2 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 34861640]
SJSA-1	IC₅₀	62.2 nM Compound: (R)-8i	Antiproliferative activity against human SJSA-1 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human SJSA-1 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 34861640]
SJSA-1	IC₅₀	62.2 nM Compound: (R)-8i	Antiproliferative activity against human SJSA-1 cells with increase MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SJSA-1 cells with increase MYOF expression assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 34861640]
SW1353	IC₅₀	19.9 nM Compound: (R)-8i	Antiproliferative activity against human SW1353 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human SW1353 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 34861640]
U2OS	IC₅₀	26.5 nM Compound: (R)-8i	Antiproliferative activity against human U2OS cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human U2OS cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 34861640]

In Vitro

Antitumor agent-51 (compound R-8i) (0-20 μM; 72 hours) selectively inhibits MNNG/HOS OS cells proliferation with IC₅₀=21.9 nM, and has much less inhibitory activity on two normal BMSC and GES1 cells (IC₅₀>10 μM)^[1].
Antitumor agent-51 (5 nM; 24 hours) induces a cell cycle arrest in MNNG/HOS cells with a 23% increase in G0/G1 phase, but no apparent cell apoptosis^[1].
Antitumor agent-51 (5 and 20 nM; 24 hours) significantly suppresses the migration of MNNG/HOS cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:

MNNG/HOS, MG63, SJSA-1, U2OS, 143B, SAOS-2, HOS, SW1353, GES1, and BMSC cells^[1]
Concentration:

0-20 μM
Incubation Time:

72 hours
Result:

Selectively inhibited MNNG/HOS cells proliferation with IC₅₀=21.9 nM, and showed much less inhibitory activity on two normal BMSC and GES1 cells (IC₅₀>10 μM).

Cell Cycle Analysis

Cell Line:

MNNG/HOS cells^[1]
Concentration:

5 nM
Incubation Time:

24 hours
Result:

Induced a cell cycle arrest with a 23% increase in G0/G1 phase, but no apparent cell apoptosis.

In Vivo

Antitumor agent-51 (12.5 or 62.5 mg/kg; i.p. or i.v., single) exhibits good intraperitoneal plasma exposures (AUC_0-∞>6900 h ng/mL) and an acceptable bioavailability (52.1%) for the i.p. administration in male ICR mice^[1].
Antitumor agent-51 (62.5 mg/kg; i.p., twice per day for 18 days) significantly suppresses MNNG/HOS tumor growth with tumor growth inhibition (TGI) of 52.9% and does not induce an obvious toxicity in nude mice^[1].
Pharmacokinetic Parameters of Antitumor agent-51 in male ICR mice^[1].

	IV (12.5 mg/kg)	IP (62.5 mg/kg)
T_1/2 (h)	0.061	0.641
AUC_0-inf (h·ng/mL)	3230	8406
C_max (ng/mL)		20511
CL (mL/min/kg)	66.9
F (%)		52.1

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male ICR mice (30 g, n=3)^[1]
Dosage:

12.5 or 62.5 mg/kg
Administration:

i.p. or i.v., single (Pharmacokinetic Analysis)
Result:

Showed good intraperitoneal plasma exposures (AUC_0-∞ > 6900 h ng/mL) and an acceptable bioavailability (52.1%) for the i.p. administration.

Animal Model:

Female BALB/c nude mice (3 months, human MNNG/HOS xenografts)^[1]
Dosage:

62.5 mg/kg
Administration:

i.p., twice per day for 18 days
Result:

Significantly suppressed MNNG/HOS tumor growth with tumor growth inhibition (TGI) of 52.9% and did not induce an obvious toxicity.

Chemical Information

CAS No. 3035774-65-0
Molecular Weight 435.54
Formula C₂₃H₂₅N₅O₂S
SMILES

CC1=CC(N2C(CS[C@@H]2C3=CC(C(NCCCCN4C=CC=N4)=O)=CC=C3)=O)=NC=C1
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Deng Y, et al. Novel 2-phenyl-3-(Pyridin-2-yl) thiazolidin-4-one derivatives as potent inhibitors for proliferation of osteosarcoma cells in vitro and in vivo. Eur J Med Chem. 2022;228:114010. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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