ARB-272572
Based on 1 Customer Validation
ARB-272572 is an oral effective small molecule PD-L1 inhibitor, with an IC50 value of 400 pM. ARB-272572 has research significance in tumors and chronic viral infections.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.96%
- CAS No.: 2368182-63-0
- Formule: C32H36N6O4
- Masse moléculaire:568.67
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Jurkat | EC50 |
14.7 nM
Compound: Cmpd A
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Inhibition of interaction of human PD-1 expressed in Jurkat T cells co-transfected with NFAT response element/human PD-L1 expressed in CHO-K1 cells co-expressing cell surface protein and TCR ligand preincubated with CHO-K1 cells followed by Jurkat cell ad
Inhibition of interaction of human PD-1 expressed in Jurkat T cells co-transfected with NFAT response element/human PD-L1 expressed in CHO-K1 cells co-expressing cell surface protein and TCR ligand preincubated with CHO-K1 cells followed by Jurkat cell ad
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[PMID: 38894909] |
| Jurkat | EC50 |
17 nM
Compound: Cmpd A
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Inhibition of interaction of PD-1 (unknown origin) expressed in Jurkat T cells co-transfected with NFAT response element/PD-L1 (unknown origin) expressed in CHO-K1 cells by reporter bioassay
Inhibition of interaction of PD-1 (unknown origin) expressed in Jurkat T cells co-transfected with NFAT response element/PD-L1 (unknown origin) expressed in CHO-K1 cells by reporter bioassay
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[PMID: 38894909] |
In Vitro
ARB-272572 inhibits PD-1/PD-L1 in PD-L1 aAPC/CHO-K1 cells, with an IC50 of 17 nM[1].
ARB-272572 boosts IFNγ expression in the CMV recall assay, with an IC50 of 3 nM[1].
ARB-272572 (0.3-10 μM, 1 h) suppresses the PD-1/PD-L1 immune checkpoint axis in aAPC/CHO-K1 cells by inducing PD-L1 internalization, showing immunomodulatory effects similar to those of anti-PD-L1 antibodies[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PD-L1 aAPC/CHO-K1
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Concentration:0.3, 1, 3, 10 μM
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Incubation Time:1 h
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Result:Caused PD-L1 to shift to a higher molecular weight form.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Humanized mouse model of colon cancer [1]
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Dosage:10 mg/kg; daily; 7 days
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Administration:Oral
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Result:Reduced tumor volume, tumor regression, and the number of CD3+ T cells in peripheral blood increased, especially CD4+ T cells significantly increased, while the proportion of regulatory T cells decreased significantly.
Chemical Information
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CAS No. 2368182-63-0
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Appearance Solid
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Masse moléculaire 568.67
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Formule C32H36N6O4
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Color White to off-white
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SMILES
CC1=C(C=CC=C1C2=CC=CC(NC(C3=NC=C(C=C3)CNCCO)=O)=C2C)NC(C4=CC=C(C=N4)CNCCO)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (175.85 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)
In Vivo:
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: ≥ 2.08 mg/mL (3.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (3.66 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (270 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Park JJ, et al. Checkpoint inhibition through small molecule-induced internalization of programmed death-ligand 1. Nat Commun. 2021 Feb 22;12(1):1222. [Content Brief]
[2]. Zhijie Wang, et al. Reducing PD-L1 Expression by Degraders and Downregulators as a Novel Strategy to Target the PD-1/PD-L1 Pathway. J Med Chem. 2024 Apr 25;67(8):6027-6043. [Content Brief]
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 | 1.7585 mL | 8.7924 mL | 17.5849 mL | 43.9622 mL |
| 5 mM | 0.3517 mL | 1.7585 mL | 3.5170 mL | 8.7924 mL | |
| 10 mM | 0.1758 mL | 0.8792 mL | 1.7585 mL | 4.3962 mL | |
| 15 mM | 0.1172 mL | 0.5862 mL | 1.1723 mL | 2.9308 mL | |
| 20 mM | 0.0879 mL | 0.4396 mL | 0.8792 mL | 2.1981 mL | |
| 25 mM | 0.0703 mL | 0.3517 mL | 0.7034 mL | 1.7585 mL | |
| 30 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4654 mL | |
| 40 mM | 0.0440 mL | 0.2198 mL | 0.4396 mL | 1.0991 mL | |
| 50 mM | 0.0352 mL | 0.1758 mL | 0.3517 mL | 0.8792 mL | |
| 60 mM | 0.0293 mL | 0.1465 mL | 0.2931 mL | 0.7327 mL | |
| 80 mM | 0.0220 mL | 0.1099 mL | 0.2198 mL | 0.5495 mL | |
| 100 mM | 0.0176 mL | 0.0879 mL | 0.1758 mL | 0.4396 mL |
ARB-272572 Related Classifications
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