PARP7-IN-22
Based on 1 Customer Validation
PARP7-IN-22 (XLY-1) is a PARP7 inhibitor with an IC50 of 0.6 nM. PARP7-IN-22 (XLY-1) is orally active, enhances type I interferon signaling in vitro, restores type I interferon signaling, promotes T cell infiltration into tumor tissues, and significantly inhibits tumor growth. PARP7-IN-22 shows promise for research in the field of cancer immunotherapy.
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- Purity: 99.59%
- CAS No.: 2946705-91-3
- 화학식: C19H22F6N8O2
- 분자량:508.42
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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PARP-7 0.6 nM (IC50) |
PARP7-IN-22 (XLY-1) (5μM-20μM, 14 days) demonstrates no substantial influence on the activity of CT26 cells[1]. PARP7-IN-22 (49 nM-4000 nM, 72 h) significantly enhances the expression of IFN-β and CXCL10, as well as the phosphorylation of STAT1, in a dose-dependent manner [1]. PARP7-IN-22 (49 nM-4000 nM, 72 h) administration exhibites a noticeable increase in TBK1 phosphorylation[1]. PARP7-IN-22 (49 nM-4000 nM, 72 h) effectively promotes the type I interferon signaling cascade, thereby exerting anti-tumor effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CT26 cells
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Concentration:49 nM-4000 nM
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Incubation Time:72 h
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Result:Resulted in a gradual increase in the mRNA levels of IFN-β and CXCL10 as the dose ranged from 49 nM to 4000 nM.
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Cell Line:CT26 cells
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Concentration:49 nM-4000 nM
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Incubation Time:72 h
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Result:Resulted in a dose-dependent increase in the protein levels of STAT1 and TBK1, with STAT1 protein levels showing a dose-dependent increase in the range of 49 nM to 4000 nM.
Pharmacokinetic Analysis in CT26 Syngeneic Model[1]
| PARP7-IN-22 (XLY-1) | T1/2 (h) | Tmax (h) | Cmax(g/mL) | C0(g/mL) | AUC0-∞ (h ng/mL) | Vz (L/kg) | CL (L/h/kg) | MRT0-∞(h) | F (%) |
| i.v. (5 mg/kg) | 5.42 | 1.25 | 353.80 | 1632.80 | 1626.00 | 0.029 | 0.004 | 3.22 | - |
| p.o. (30 mg/kg) | 5.52 | 1.75 | 674.00 | - | 2368.10 | 0.112 | 0.014 | 4.84 | 24.27 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2946705-91-3
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Appearance Solid
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분자량 508.42
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화학식 C19H22F6N8O2
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Color White to off-white
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SMILES
O=C1NN=CC(NCCCCNC(N2CCN(CC2)C3=NC=C(C(F)(F)F)C=N3)=O)=C1C(F)(F)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (196.69 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. 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. 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 1.9669 mL | 9.8344 mL | 19.6688 mL | 49.1719 mL |
| 5 mM | 0.3934 mL | 1.9669 mL | 3.9338 mL | 9.8344 mL | |
| 10 mM | 0.1967 mL | 0.9834 mL | 1.9669 mL | 4.9172 mL | |
| 15 mM | 0.1311 mL | 0.6556 mL | 1.3113 mL | 3.2781 mL | |
| 20 mM | 0.0983 mL | 0.4917 mL | 0.9834 mL | 2.4586 mL | |
| 25 mM | 0.0787 mL | 0.3934 mL | 0.7868 mL | 1.9669 mL | |
| 30 mM | 0.0656 mL | 0.3278 mL | 0.6556 mL | 1.6391 mL | |
| 40 mM | 0.0492 mL | 0.2459 mL | 0.4917 mL | 1.2293 mL | |
| 50 mM | 0.0393 mL | 0.1967 mL | 0.3934 mL | 0.9834 mL | |
| 60 mM | 0.0328 mL | 0.1639 mL | 0.3278 mL | 0.8195 mL | |
| 80 mM | 0.0246 mL | 0.1229 mL | 0.2459 mL | 0.6146 mL | |
| 100 mM | 0.0197 mL | 0.0983 mL | 0.1967 mL | 0.4917 mL |
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