PD-1/PD-L1-IN-9
Based on 2 publication(s) in Google Scholar
PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model.
For research use only. We do not sell to patients.
- Purity: 99.59%
- CAS No.: 2628506-54-5
- Formula: C22H24N2O2
- Molecular Weight:348.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Publications Citing Use of MedChemExpress (MCE) PD-1/PD-L1-IN-9
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Biological Activity
IC50: 3.8 nM (PD-1/PD-L1)[1]
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-231 | EC50 |
100 nM
Compound: 24
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Antitumor immunity against human MDA-MB-231 cells co-cultured with CD3/CD28/CD2 T cell activator stimulated human PMBC assessed as cell death measuring lactate dehydrogenase release measured for 12 hrs by PBMC killing assay
Antitumor immunity against human MDA-MB-231 cells co-cultured with CD3/CD28/CD2 T cell activator stimulated human PMBC assessed as cell death measuring lactate dehydrogenase release measured for 12 hrs by PBMC killing assay
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[PMID: 34056906] |
PD-1/PD-L1-IN-9 (compound 24) (46.9-1500 nM; pretreated for 2 h) dose-dependently significantly activates the antitumor immunity of peripheral blood mononuclear cells (PBMCs) to MDB-MB 231 cells, with an EC50 of ∼100 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PD-1/PD-L1-IN-9 (3 mg/kg; i.v.; single dose) exhibits half-life (T1/2=4.2 h), plasma clearance (Cl=11.5 L/h/kg) and Cmax (1233 ng/mL) in rats[1].
PD-1/PD-L1-IN-9 (25 mg/kg; p.o.; single dose) exhibits moderate oral bioavailability (F=22 %), half-life (t1/2=6.4 h) and Cmax (192 ng/mL) in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice (5-6 weeks) were inoculated CT26 cells[1]
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Dosage:40 mg/kg, 80 mg/kg
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Administration:Oral gavage; once daily, for 2 weeks
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Result:Significantly decreased the final tumor weight, with TGI values of 60 and 67% at the dose of 40 and 80 mg/kg, respectively.
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Animal Model:Pharmacokinetic analysis in sprague-Dawley (SD) rats[1]
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Dosage:3 mg/kg and 25 mg/kg
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Administration:Intravenous injection or oral gavage; single dose
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Result:
Route Dose (mg/kg) AUC(0-t) (ng·h/mL) Cmax (ng/mL) t1/2 (h) Tmax Cl (L·h/kg) Vz (L/kg) F (%) i.v. 3 430.5 1233 4.2 0.03 11.5 78.6 / p.o. 25 787.4 192 6.4 0.69 28.8 249.3 22
Chemical Information
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CAS No. 2628506-54-5
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Appearance Solid
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Molecular Weight 348.44
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Formula C22H24N2O2
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Color White to off-white
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SMILES
CC1=C(C=CC=C1C2=CC=CC=C2)C3=NC(OC)=C(C=C3)CNCCO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Biochim Biophys Acta Mol Basis Dis
Combined cryoablation and PD-1 inhibitor synergistically enhance antitumor immune responses in Lewis lung adenocarcinoma mice via the PI3K/AKT/mTOR pathway. [Abstract]2024 Oct;1870(7):167262. PMID: 38815768 -
Int J Hyperthermia
Cryoablation combined with programmed cell death protein 1 (PD-1) inhibitors regulates myeloid-derived suppressor cells (MDSCs) through the JAK2-STAT3-S100A8/A9 axis in mice with Lewis lung carcinoma. [Abstract]2025 Dec;42(1):2525444. PMID: 40734480
Solvent & Solubility
DMSO : 100 mg/mL (286.99 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 (7.17 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 (7.17 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.
Purity & Documentation
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Data Sheet (275 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 | 2.8699 mL | 14.3497 mL | 28.6993 mL | 71.7484 mL |
| 5 mM | 0.5740 mL | 2.8699 mL | 5.7399 mL | 14.3497 mL | |
| 10 mM | 0.2870 mL | 1.4350 mL | 2.8699 mL | 7.1748 mL | |
| 15 mM | 0.1913 mL | 0.9566 mL | 1.9133 mL | 4.7832 mL | |
| 20 mM | 0.1435 mL | 0.7175 mL | 1.4350 mL | 3.5874 mL | |
| 25 mM | 0.1148 mL | 0.5740 mL | 1.1480 mL | 2.8699 mL | |
| 30 mM | 0.0957 mL | 0.4783 mL | 0.9566 mL | 2.3916 mL | |
| 40 mM | 0.0717 mL | 0.3587 mL | 0.7175 mL | 1.7937 mL | |
| 50 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4350 mL | |
| 60 mM | 0.0478 mL | 0.2392 mL | 0.4783 mL | 1.1958 mL | |
| 80 mM | 0.0359 mL | 0.1794 mL | 0.3587 mL | 0.8969 mL | |
| 100 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7175 mL |
PD-1/PD-L1-IN-9 Related Classifications
HY-132192 Related Classifications
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