PD-1/PD-L1-IN-9 hydrochloride
Based on 4 publication(s) in Google Scholar
PD-1/PD-L1-IN-9 hydrochloride 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 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model.
For research use only. We do not sell to patients.
- Purity : 98.59%
- Formula: C22H25ClN2O2
- Molecular Weight:384.90
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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)
Publications Citing Use of MedChemExpress (MCE) PD-1/PD-L1-IN-9 hydrochloride
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Biological Activity
Description
In Vitro
PD-1/PD-L1-IN-9 hydrochloride (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.
In Vivo
PD-1/PD-L1-IN-9 hydrochloride (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 hydrochloride (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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Appearance Solid
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Molecular Weight 384.90
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Formula C22H25ClN2O2
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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.[H]Cl
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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)
Publications (4)
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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 -
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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
In Vitro:
DMSO : 125 mg/mL (324.76 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 (273 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 (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 | 2.5981 mL | 12.9904 mL | 25.9808 mL | 64.9519 mL |
| 5 mM | 0.5196 mL | 2.5981 mL | 5.1962 mL | 12.9904 mL | |
| 10 mM | 0.2598 mL | 1.2990 mL | 2.5981 mL | 6.4952 mL | |
| 15 mM | 0.1732 mL | 0.8660 mL | 1.7321 mL | 4.3301 mL | |
| 20 mM | 0.1299 mL | 0.6495 mL | 1.2990 mL | 3.2476 mL | |
| 25 mM | 0.1039 mL | 0.5196 mL | 1.0392 mL | 2.5981 mL | |
| 30 mM | 0.0866 mL | 0.4330 mL | 0.8660 mL | 2.1651 mL | |
| 40 mM | 0.0650 mL | 0.3248 mL | 0.6495 mL | 1.6238 mL | |
| 50 mM | 0.0520 mL | 0.2598 mL | 0.5196 mL | 1.2990 mL | |
| 60 mM | 0.0433 mL | 0.2165 mL | 0.4330 mL | 1.0825 mL | |
| 80 mM | 0.0325 mL | 0.1624 mL | 0.3248 mL | 0.8119 mL | |
| 100 mM | 0.0260 mL | 0.1299 mL | 0.2598 mL | 0.6495 mL |