N-(吡啶-3-基)噻吩-2-羧酰胺

生物活性体外研究体内研究 N-(吡啶-3-基)噻吩-2-羧酰胺试剂级价格

N-(吡啶-3-基)噻吩-2-羧酰胺

CAS号:62289-81-0
英文名:N-pyridin-3-ylthiophene-2-carboxamide
中文名:N-(吡啶-3-基)噻吩-2-羧酰胺
CBNumber:CB14316832
分子式:C10H8N2OS
分子量:204.25
MOL File:62289-81-0.mol

N-(吡啶-3-基)噻吩-2-羧酰胺化学性质

沸点 :270.8±15.0 °C(Predicted)
密度 :1.352±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: 100 mg/mL (489.60 mM)
酸度系数(pKa) :12.39±0.70(Predicted)
形态 :Solid
颜色 :Off-white to light yellow

N-(吡啶-3-基)噻吩-2-羧酰胺性质、用途与生产工艺

生物活性 SW106065 是恶性周围神经鞘瘤 (MPNST) 的凋亡 (apoptosis) 诱导剂。SW106065 以 EC50 为 1 µM 来抑制 sMPNST 细胞和其他模型中 MPNST 的 ATP 消耗。SW106065 可用于 MPNST 的研究。

体外研究

SW106065 (Compound 21, Cpd21) inhibits the human MPNST cell lines growth in a dose-dependent manner, and EC ₅₀ concentrations of 439 nM and 753.6 nM for S462 and SNF96.2 cells, respectively. SW106065 remains nontoxic to normally dividing Schwann cells or mouse embryonic fibroblasts.
SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment shows a decreased percentage of cells in S phase, and a corresponding increased percentage in G1/G0 and G2/M.
SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment decreases the levels of cyclin A2, cyclin B1, cyclin D1, cyclin E, cdk4, and cdk6. And increases levels of cdkn1a and cdkn2a mRNA were observed in a dose-dependent manner. SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment decreases the levels of Cyclin D1 protein.
SW106065 (Cpd21) treatment significant increase in the percentage of apoptotic cells.

Cell Cycle Analysis

Cell Line:	sMPNST cells
Concentration:	0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM
Incubation Time:	24 hours
Result:	Showed a decreased percentage of cells in S phase, and a corresponding increased percentage in G1/G0 and G2/M.

RT-PCR

Cell Line:	sMPNST cells
Concentration:	0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM
Incubation Time:	24 hours
Result:	Decreased levels of cyclin A2, cyclin B1, cyclin D1, cyclin E, cdk4, and cdk6. Increased levels of cdkn1a and cdkn2a mRNA were observed in a dose-dependent manner.

Western Blot Analysis

Cell Line:	sMPNST cells
Concentration:	0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM
Incubation Time:	24 hours
Result:	Decreased levels of Cyclin D1 protein.

体内研究

SW106065 (Cpd21; 40 mg/kg; intraperitoneal injection; twice per day for 4 weeks) treatment can be delivered to mice in concentrations to sufficiently penetrate sMPNST tissue, and inhibit tumor development.

Animal Model:	NCR-nu/nu female mice (6-7 week old) injected with MPNST cells
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; twice per day for 4 weeks
Result:	Reduced MPNST burden in a mouse allograft model.