2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. Spiclomazine hydrochloride

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

Cat. No.: HY-122152
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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.

Spiclomazine hydrochloride Chemical Structure

Spiclomazine hydrochloride Chemical Structure

CAS No. : 27007-85-8

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Spiclomazine hydrochloride Related Antibodies

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Description

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

 

In Vitro

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.

Spiclomazine hydrochloride Related Antibodies

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.
In Vivo

Spiclomazine (68 mg/kg; i.p.; every other day for two weeks) hydrochloride reduces the growth of MIA PaCa-2 xenograft in mice[2].

MedChemExpress (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.
Molecular Weight

482.49

Formula

C22H25Cl2N3OS2
CAS No.
SMILES

O=C1CSC2(N1)CCN(CC2)CCCN3C4=C(SC5=CC=C(C=C35)Cl)C=CC=C4.[H]Cl
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Spiclomazine hydrochloride Related Classifications

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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.

Keywords:

Spiclomazine27007-85-8APY-606ClospirazineAPY606APY 606RasantipsychoticantitumorCFPAC-1MIA PaCa-2Inhibitorinhibitorinhibit

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