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Spiclomazine hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Spiclomazine hydrochloride图片
CAS NO:27007-85-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
APY-606
Clospirazine hydrochloride
产品介绍
Spiclomazine hydrochloride (APY-606) 是一种抗精神病药和抗肿瘤药。Spiclomazine hydrochloride 抑制KRas。Spiclomazine hydrochloride 诱导癌细胞凋亡(apoptosis)。
生物活性

Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibitsKRas. Spiclomazine hydrochloride inducescancercellapoptosis[1][2].

IC50& Target[2]

K-RAS

 

体外研究
(In Vitro)

Spiclomazine (0-100 μg/mL; 24 and 48 h) hydrochloride 以剂量依赖的方式抑制胰腺癌细胞的非接触集落形成[1]
Spiclomazine (0.5x and 1x IC50; 48 h) hydrochloride 通过线粒体途径诱导 CFPAC-1 和 MIA PaCa-2 细胞凋亡,显著提高细胞内 ROS 水平[1]
Spiclomazine (30 μg/mL; 24 h) hydrochloride 抑制 CFPAC-1 和 MIA PaCa-2 细胞的细胞运动性[1]
Spiclomazine (10 and 20 μg/mL; 24 h) hydrochloride 在 G2 期时阻滞癌细胞周期进展[2]

Cell Viability Assay[1]

Cell Line:CFPAC-1, MIA PaCa-2, HEK-293 and HL-7702 cells
Concentration:0-100 μg/mL
Incubation Time:24 and 48 h
Result:Resulted in a time and dose-dependent growth reduction of CFPAC-1 and MIA PaCa-2 cells. Exhibited less cytotoxicity to normal HEK-293 and HL-7702 cells. The IC50for 48 h treatment was 15.2±2.0 μg/mL (31.5±2.0 μM) for CFPAC-1, 12.9±0.9 μg/mL (26.8±0.9 μM) for MIA PaCa-2, 41.9±1.4 μg/mL (86.9±1.4 μM) for HEK-293, and 71.2±3.3 μg/mL (147.7±3.3 μM) for HL-7702, respectively.

Apoptosis Analysis[1]

Cell Line:CFPAC-1 and MIA PaCa-2 cells
Concentration:7.6 and 15.2 μg/mL for CFPAC-1, 6.45 and 12.9 μg/mL for MIA PaCa-2
Incubation Time:48 h
Result:Increased early apoptotic cells.

Western Blot Analysis[1]

Cell Line:CFPAC-1 and MIA PaCa-2 cells
Concentration:10, 20 and 30 μg/mL
Incubation Time:24 h
Result:The cleavages of caspase-3/9 were increased in a dose-dependent manner. The expression of Bax was up-regulated concomitant with the related attenuation of Bcl-2 protein expression. The level of cytochrome c in cytosol was increased accompanied by the decrease of the level of cytochrome c in mitochondria.

Cell Migration Assay[1]

Cell Line:CFPAC-1 and MIA PaCa-2 cells
Concentration:30 μg/mL
Incubation Time:24 h
Result:Markedly suppressed the migration of both pancreatic carcinoma cells.

Cell Invasion Assay[1]

Cell Line:CFPAC-1 and MIA PaCa-2 cells
Concentration:30 μg/mL
Incubation Time:24 h
Result:Suppressed the invasion by down-regulating the expression of MMP-2/9.

Cell Cycle Analysis[2]

Cell Line:MIA PaCa-2, CFPAC-1, BxPC-3, Capan-1 and SW1990 cells
Concentration:10 and 20 μg/mL
Incubation Time:24 h
Result:Promoted cancer cell cycle arrest at either G2 phase in MIA PaCa-2, CFPAC-1, and BxPC-3 cell lines or S phase in Capan-1 and SW1990 cell lines.
体内研究
(In Vivo)

Spiclomazine (68 mg/kg; i.p.; every other day for two weeks) hydrochloride 降低小鼠 MIA PaCa-2 异种移植肿瘤的生长[2]

Animal Model:BALB/c mice, MIA PaCa-2 xenograft model[2]
Dosage:68 mg/kg
Administration:Intraperitoneal injection, every other day for two weeks
Result:Completely blocked the growth of tumors in three of the five mice.
分子量

482.49

Formula

C22H25Cl2N3OS2

CAS 号

27007-85-8

中文名称

螺氯马嗪

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.