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  3. Spiclomazine hydrochloride

Spiclomazine hydrochloride  (Synonyms: APY-606; Clospirazine hydrochloride)

目录号: HY-122152
产品使用指南

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)。

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Spiclomazine hydrochloride Chemical Structure

Spiclomazine hydrochloride Chemical Structure

CAS No. : 27007-85-8

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Spiclomazine hydrochloride 的其他形式现货产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis[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]

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

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 IC50 for 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]

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

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
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.

纯度 & 产品资料
参考文献
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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Spiclomazine hydrochloride
目录号:
HY-122152
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