store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
1 mg | 在庫あり | ¥ 73,500 |
25 mg | 約6-8 週間 | ¥ 248,000 |
50 mg | 約6-8 週間 | ¥ 323,500 |
100 mg | 約6-8 週間 | ¥ 509,500 |
説明 | 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. |
ターゲット&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]. |
別名 | SMOCL-9112 |
分子量 | 486.42 |
分子式 | C23H18F4N6O2 |
CAS No. | 1551355-46-4 |
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 80 mg/mL(164.47 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Simmiparib 1551355-46-4 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair PARP SMOCL-9112 Inhibitor inhibitor inhibit