Spiclomazine hydrochloride
Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis.
For research use only. We do not sell to patients.
- CAS No.: 27007-85-8
- Formula: C22H25Cl2N3OS2
- Molecular Weight:482.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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K-RAS |
Spiclomazine (0-100 μg/mL; 24 and 48 h) hydrochloride inhibits contact-independent colony formation of pancreatic carcinoma cells in a dose-dependent manner[1].
Spiclomazine (0.5x and 1x IC50; 48 h) hydrochloride induces CFPAC-1 and MIA PaCa-2 cells apoptosis in the mitochondrial pathway, and significantly enhanced intracellular ROS level[1].
Spiclomazine (30 μg/mL; 24 h) hydrochloride suppresses cellular motility in CFPAC-1 and MIA PaCa-2 cells[1].
Spiclomazine (10 and 20 μg/mL; 24 h) hydrochloride arrests cancer cell cycle progression at G2 phase[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CFPAC-1, MIA PaCa-2, HEK-293 and HL-7702 cells
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Concentration:0-100 μg/mL
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Incubation Time:24 and 48 h
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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.
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Cell Line:CFPAC-1 and MIA PaCa-2 cells
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Concentration:7.6 and 15.2 μg/mL for CFPAC-1, 6.45 and 12.9 μg/mL for MIA PaCa-2
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Incubation Time:48 h
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Result:Increased early apoptotic cells.
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Cell Line:CFPAC-1 and MIA PaCa-2 cells
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Concentration:10, 20 and 30 μg/mL
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Incubation Time:24 h
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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.
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Cell Line:CFPAC-1 and MIA PaCa-2 cells
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Concentration:30 μg/mL
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Incubation Time:24 h
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Result:Markedly suppressed the migration of both pancreatic carcinoma cells.
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Cell Line:CFPAC-1 and MIA PaCa-2 cells
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Concentration:30 μg/mL
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Incubation Time:24 h
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Result:Suppressed the invasion by down-regulating the expression of MMP-2/9.
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Cell Line:MIA PaCa-2, CFPAC-1, BxPC-3, Capan-1 and SW1990 cells
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Concentration:10 and 20 μg/mL
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Incubation Time:24 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice, MIA PaCa-2 xenograft model[2]
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Dosage:68 mg/kg
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Administration:Intraperitoneal injection, every other day for two weeks
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Result:Completely blocked the growth of tumors in three of the five mice.
Chemical Information
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CAS No. 27007-85-8
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Molecular Weight 482.49
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Formula C22H25Cl2N3OS2
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SMILES
O=C1CSC2(N1)CCN(CC2)CCCN3C4=C(SC5=CC=C(C=C35)Cl)C=CC=C4.[H]Cl
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Synonyms
APY-606; Clospirazine hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Zhao W, et al. Spiclomazine induces apoptosis associated with the suppression of cell viability, migration and invasion in pancreatic carcinoma cells. PLoS One. 2013 Jun 20;8(6):e66362. [Content Brief]
[2]. Guo X, et al. Spiclomazine displays a preferential anti-tumor activity in mutant KRas-driven pancreatic cancer. Oncotarget. 2018 Jan 8;9(6):6938-6951. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Spiclomazine hydrochloride Related Classifications
HY-122152 Related Classifications
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