Antitumor agent-51

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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

Antitumor agent-51 Chemical Structure

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

* Please select Quantity before adding items.

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].

Shanghai Jinpan Biotech Co Ltd 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 (AUC0-∞>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)
T1/2 (h) 0.061 0.641
AUC0-inf (h·ng/mL) 3230 8406
Cmax (ng/mL) 20511
CL (mL/min/kg) 66.9
F (%) 52.1

Shanghai Jinpan Biotech Co Ltd 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 (AUC0-∞ > 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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务