Antitumor agent-51 | whatman (沃特曼)

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Antitumor agent-51

Antitumor agent-51 对骨肉瘤细胞的生长和迁移具有有效的选择性抑制作用，对 MNNG/HOS 细胞的 IC₅₀ 为 21.9 nM。Antitumor agent-51 具有低毒性和相当大的生物利用度。

Antitumor agent-51 Chemical Structure

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

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生物活性

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^[1].

IC₅₀ & Target

IC₅₀: 21.9 nM in MNNG/HOS cells^[1]

体外研究
(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].

上海金畔生物科技有限公司 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.

体内研究
(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

上海金畔生物科技有限公司 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.

分子量

435.54

Formula

C₂₃H₂₅N₅O₂S

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]. 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.

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