PARP1/NAMPT-IN-1
Based on 1 Customer Validation
PARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC50 values of 1.2 nM and 6.7 nM, respectively. PARP1/NAMPT-IN-1 can disrupt the homologous recombination repair (HRR) pathway, leading to the accumulation of DNA double-strand breaks (DSBs), inducing cell cycle arrest and apoptosis, and also has antimigratory effects. PARP1/NAMPT-IN-1 exhibits excellent antitumor effects in a breast cancer xenograft model. PARP1/NAMPT-IN-1 can be used for the study of triple-negative breast cancer (TNBC).
For research use only. We do not sell to patients.
- Purity: 98.45%
- CAS No.: 3084810-86-3
- Formula: C35H31FN6O3
- Molecular Weight:602.66
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
PARP1 1.2 nM (IC50) |
NAMPT 6.7 nM (IC50) |
In Vitro
PARP1/NAMPT-IN-1 (compound 10 n) (24 h-7 days) shows selective antiproliferative activity against MDA-MB-231 cells (IC50 = 1.28 nM) and MDA-MB-468 cells (IC50 = 0.46 nM). PARP1/NAMPT-IN-1 shows the negligible cytotoxic effects (IC50 > 20 μM) against MCF-10A cells[1].
PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) induces cell cycle arrest and apoptosis in MDA-MB-231 cells[1].
PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) disrupts HRR pathway to induce synthetic lethality and rrigger DSBs in MDA-MB-231 cells[1].
PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) exhibits marked antimigratory effects in MDA-MB-231 cells[1].
PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) significantly increases cGAS level and phosphorylation of STING, TBK1, and IRF3 in 4T1 cells in vitro, suggesting its intratumoral activation of STING signaling pathway[1].
PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) enhances TBK1 and IRF3 phosphorylation in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Dose-dependently arrested MDA-MB-231 cells at G2/M phase with a low concentration (0.3 μM).
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Cell Line:MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Induced a dose-dependent increase in apoptosis.
Upregulated pro-apoptotic Bax and cleaved PARP while downregulating antiapoptotic Bcl-2.
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Cell Line:MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Induced significantly higher nuclear γH2AX levels.
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Cell Line:MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Significantly suppressed expression of all tested HRR components (BRCA1, CtIP, Mre11, RAD51, p-RPA32).
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Cell Line:MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Inhibited MDA-MB-231 cell migration.
Potently downregulated the promigratory markers MMP2 and N-cadherin (typically elevated in epithelial-mesenchymal transition (EMT)) while upregulating E-cadherin (an epithelial marker associated with reduced motility that is frequently lost in EMT).
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Cell Line:4T1 cells and MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Significantly increased cGAS level and phosphorylation of STING, TBK1, and IRF3 in 4T1 cells.
Enhanced TBK1 and IRF3 phosphorylation in MDA-MB-231 cells.
In Vivo
PARP1/NAMPT-IN-1 (5 mg/kg; i.p.; once a day; for 5 days) effectively inhibits in 4T1 mouse xenograft models[1].
PARP1/NAMPT-IN-1 (5 mg/kg; i.p.; once a day; for 14 days) activates the STING pathway to drive antitumor immunity in 4T1murine BRCA wild-Type TNBC model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice (6-8 weeks old), received subcutaneous injections of MDA-MB-231 cells (5 × 106 cells per mouse in 0.1 mL PBS) in the right flank[1].
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Dosage:5 mg/kg, or 10 mg/kg
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Administration:Intraperitoneal (IP) injection; once daily; for 14 days
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Result:At 5 mg/kg achieved a notable tumor growth inhibition (TGI = 59.98%).
No significant weight loss or mortality at 5 mg/kg.
At 10 mg/kg, significantly enhanced TGI to 83.37%, while maintaining a favorable safety profile, as evidenced by no mortality and significant weight loss.
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Animal Model:Female immunocompetent BALB/c mice (6-8 weeks old) were intravenously injected with 4T1 cells (5 × 105 cells per mouse in 0.1 mL PBS)[1].
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Dosage:5 mg/kg
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Administration:Intraperitoneal (IP) injection; once daily; for 5 days
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Result:Markedly reduced the formation of lung metastatic nodules compared to the control group.
H&E staining revealing significantly fewer metastatic lesions in lung tissues.
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Animal Model:Female immunocompetent BALB/c mice (6-8 weeks old) were intravenously injected with 4T1 cells (5 × 105 cells per mouse in 0.1 mL PBS)[1].
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Dosage:5 mg/kg
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Administration:Intraperitoneal (IP) injection; once daily; for 14 days
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Result:Demonstrated excellent antitumor efficacy (TGI = 70.18%) without significant weight loss or mortality.
Significantly reduced proliferation (Ki67 IHC) and caused extensive tissue destruction (H&E).
Markedly increased tumor-infiltrating CD3+ and CD8+ T cells.
Suppressed the recruitment of MDSCs, evidenced by reduced coexpression of CD11b and Ly6G in multiplex immunofluorescence staining.
Significantly elevated cGAS levels and phosphorylation of STING, TBK1, and IRF3.
Chemical Information
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CAS No. 3084810-86-3
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Appearance Solid
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Molecular Weight 602.66
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Formula C35H31FN6O3
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Color White to off-white
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SMILES
O=C1C2=CC=CC=C2C(CC3=CC(C(N4CCC(CC4)C5=CC=C(C=C5)NC(N6CC7=C(C6)C=NC=C7)=O)=O)=C(C=C3)F)=NN1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (82.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6593 mL | 8.2966 mL | 16.5931 mL | 41.4828 mL |
| 5 mM | 0.3319 mL | 1.6593 mL | 3.3186 mL | 8.2966 mL | |
| 10 mM | 0.1659 mL | 0.8297 mL | 1.6593 mL | 4.1483 mL | |
| 15 mM | 0.1106 mL | 0.5531 mL | 1.1062 mL | 2.7655 mL | |
| 20 mM | 0.0830 mL | 0.4148 mL | 0.8297 mL | 2.0741 mL | |
| 25 mM | 0.0664 mL | 0.3319 mL | 0.6637 mL | 1.6593 mL | |
| 30 mM | 0.0553 mL | 0.2766 mL | 0.5531 mL | 1.3828 mL | |
| 40 mM | 0.0415 mL | 0.2074 mL | 0.4148 mL | 1.0371 mL | |
| 50 mM | 0.0332 mL | 0.1659 mL | 0.3319 mL | 0.8297 mL | |
| 60 mM | 0.0277 mL | 0.1383 mL | 0.2766 mL | 0.6914 mL | |
| 80 mM | 0.0207 mL | 0.1037 mL | 0.2074 mL | 0.5185 mL |
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