
Simmiparib
CAS No. 1551355-46-4
Simmiparib( —— )
Catalog No. M35707 CAS No. 1551355-46-4
Simmiparib (SMOCL-9112) is a novel and potent PARP1 and PARP2 inhibitor, a derivative of Olaparib.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 486 | Get Quote |
![]() ![]() |
25MG | 994 | Get Quote |
![]() ![]() |
50MG | 1297 | Get Quote |
![]() ![]() |
100MG | 1998 | Get Quote |
![]() ![]() |
500MG | Get Quote | Get Quote |
![]() ![]() |
1G | Get Quote | Get Quote |
![]() ![]() |
Biological Information
-
Product NameSimmiparib
-
NoteResearch use only, not for human use.
-
Brief DescriptionSimmiparib (SMOCL-9112) is a novel and potent PARP1 and PARP2 inhibitor, a derivative of Olaparib.
-
DescriptionSimmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts.
-
In VitroSimmiparib (0-10 μM; 3 days) exhibits anti-proliferative activity against various cancer cells.Simmiparib (0-10 μM; 48 h) induces typical G2/M arrest in Capan-1 cells.Simmiparib (0.1-2 μM; 24 h) induces apoptosis in MDA-MB-436 and V-C8 (BRCA2-/-) cells, and increases dose-dependently the levels of γH2AX.Simmiparib (1-10 μM; 48 h or 72 h) increases the phosphorylation levels of Chk1 and Chk2 and the protein levels of p-Cyclin B1 (S147), Cyclin B1, p-CDK1 (Y15) and CDK1.Cell Proliferation Assay Cell Line:Various cancer cells harboring deficient BRCA1, BRCA2, PTEN and EWS-FLI1 Concentration:0-10 μM Incubation Time:3 days Result:Exhibited anti-proliferative activity against MDA-MB-436 (BRCA1-/-), RD-ES (EWS-FLI1), DoTc2-4510 (BRCA2-/-), Capan-1 (BRCA2-/-) and U251 (PTEN-/-) with IC50s of 0.2 nM, 4.6 nM, 20 nM, 21 nM and 36 nM, respectively.Cell Cycle Analysis Cell Line:Capan-1 cell Concentration:0, 1, 3 and 10 μM Incubation Time:48 h Result:Induced typical G2/M arrest in a concentration-dependent manner.Apoptosis Analysis Cell Line:MDA-MB-436 Concentration: 0.1 and 1 μM Incubation Time:24 h Result:Led to 39.64% and 42.98% apoptosis at 0.1 and 1 μM, respectively.Increased dose-dependently the levels of γH2AX. Apoptosis Analysis Cell Line:V-C8 (BRCA2-/-) Concentration: 0.5 and 2 μM Incubation Time:24 h Result:Caused more than 57% apoptosis.Western Blot Analysis Cell Line:Capan-1 Concentration:1 and 10 μM Incubation Time:48 h or 72 h Result:Increased the phosphorylation levels of Chk1 and Chk2 but did not change the levels of the corresponding total proteins.Increased the protein levels of p-Cyclin B1 (S147), Cyclin B1, p-CDK1 (Y15) and CDK1.
-
In VivoSimmiparib (2, 4 and 8 mg/kg; p.o.; qd, for 14 days) inhibits the growth of tumor in V-C8 (BRCA2-/-) and MDA-MB-436 (BRCA2-/-) xenograft mice models.Simmiparib (10 and 50 mg/kg; p.o.; qd, for 42 days) inhibits the growth of BRCA1-mutated breast cancer in xenograft mice model.Animal Model:Female BALB/cA nude mice (Subcutaneously injected with BRCA2-/- V-C8 cells and BRCA2-/- MDA-MB-436 cells) Dosage:2, 4 and 8 mg/kg Administration:p.o.; qd, for 14 days Result:Apparently inhibited the growth of the V-C8 tumor with an inhibition rate of 74.53% at 8?mg/kg.Suppressed the growth of the BRCA1-deficient MDA-MB-436 xenografts in a dose-dependent manner with its average inhibition rates of 64.93, 82.98 and 85.79% at 2, 4 and 8?mg/kg.Did not cause significant loss of body weight.Animal Model:Female BALB/cA nude mice (Subcutaneously injected with cancer cells derived from BRCA1-mutated BR-05-0028 breast cancer tissue) Dosage:10 and 50 mg/kg Administration:p.o.; qd, for 42 days Result:Elicited dose-dependent growth inhibition with the inhibition rate of 76.73% and 93.82% at 10 mg/kg and 50 mg/kg, respectively.
-
Synonyms——
-
PathwayApoptosis
-
TargetApoptosis
-
RecptorApoptosis | PARP
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number1551355-46-4
-
Formula Weight486.42
-
Molecular FormulaC23H18F4N6O2
-
Purity>98% (HPLC)
-
SolubilityIn Vitro:?DMSO : 100 mg/mL (205.58 mM; Ultrasonic (<60°C)
-
SMILESCC1CN(Cc2nnc(n12)C(F)(F)F)C(=O)c1cc(Cc2n[nH]c(=O)c3ccccc23)ccc1F
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference



-
(Rac)-Idroxioleic ac...
Minerval is a fatty acid amide hydrolase inhibitor with anti-tumor effect.
-
Sodium taurochenodeo...
Sodium taurochenodeoxycholate is one of the main bioactive substances of animals' bile acid.?Sodium taurochenodeoxycholate induces apoptosis and shows obvious anti-inflammatory and immune regulation properties. It can increase glucose-induced insulin secretion and stimulate the electrical activity of α2-cells and enhance cytosolic Ca(2+) concentration ([Ca(2+)](c)).
-
ABT-510 acetate
ABT-510 acetate is an endogenous anti-angiogenic TSP peptide inhibitor, a thrombospondin analog, with anti-inflammatory, anti-cancer and anti-angiogenic activity that induces apoptosis and inhibits ovarian tumor growth in an orthotopic, syngeneic model of epithelial ovarian cancer.