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Simmiparib

Catalog No. T63228   CAS 1551355-46-4
Synonyms: SMOCL-9112

Simmiparib (SMOCL-9112) is a novel and potent PARP1 and PARP2 inhibitor, a derivative of Olaparib.Simmiparib induces DNA double-strand breaks (DSBs) and cell cycle arrest in homologous recombination repair (HR)-deficient cells, thereby contributing to apoptosis.Simmiparib has been used for study Parkinson's disease, Alzheimer's disease, breast cancer, and melanoma.

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Simmiparib Chemical Structure
Simmiparib, CAS 1551355-46-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 320.00
25 mg 6-8 weeks $ 1,080.00
50 mg 6-8 weeks $ 1,410.00
100 mg 6-8 weeks $ 2,220.00
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Purity: 99.51%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Simmiparib (SMOCL-9112) is a novel and potent PARP1 and PARP2 inhibitor, a derivative of Olaparib.Simmiparib induces DNA double-strand breaks (DSBs) and cell cycle arrest in homologous recombination repair (HR)-deficient cells, thereby contributing to apoptosis.Simmiparib has been used for study Parkinson's disease, Alzheimer's disease, breast cancer, and melanoma.
Targets&IC50 PARP1:0.74 nM, PARP2:0.22 nM
In vitro Simmiparib, when applied at concentrations ranging from 0 to 10 μM for 3 days, demonstrates anti-proliferative activity against various cancer cells[1].
In Capan-1 cells, Simmiparib induces typical G2/M arrest when administered at concentrations of 0-10 μM for 48 hours[1].
Apoptosis is induced in MDA-MB-436 and V-C8 (BRCA2-/-) cells by Simmiparib at concentrations of 0.1-2 μM for 24 hours. Additionally, there is a dose-dependent increase in the levels of γH2AX[1].Furthermore, treatment with Simmiparib at concentrations of 1-10 μM for 48 or 72 hours increases the phosphorylation levels of Chk1 and Chk2. Additionally, it enhances the protein levels of p-Cyclin B1 (S147), Cyclin B1, p-CDK1 (Y15), and CDK1[1].
In vivo In xenograft mouse models, Simmiparib inhibits the growth of tumors in V-C8 (BRCA2-/-) and MDA-MB-436 (BRCA2-/-) when administered orally at doses of 2, 4, and 8 mg/kg once daily for 14 days[1].Additionally, Simmiparib, at doses of 10 and 50 mg/kg administered orally once daily for 42 days, inhibits the growth of BRCA1-mutated breast cancer in xenograft mouse models[1].
Synonyms SMOCL-9112
Molecular Weight 486.42
Formula C23H18F4N6O2
CAS No. 1551355-46-4

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL(164.47 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Yuan B, et al. Poly(ADP-ribose)polymerase (PARP) inhibition and anticancer activity of simmiparib, a new inhibitor undergoing clinical trials. Cancer Lett. 2017 Feb 1;386:47-56.

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Keywords

Simmiparib 1551355-46-4 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair PARP SMOCL-9112 inhibitor inhibit

 

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