GJ19
Based on 1 Customer Validation
GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. GJ19 can effectively bind to human/murine PD-L1 protein with Kd values of 171 and 290 nM, respectively. GJ19 concentration-dependently promotes HepG2 cell mortality in a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells. GJ19 effectively suppresses tumor growth in a B16-F10 melanoma mouse model. GJ19 can be used for the study of tumor immunotherapy.
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- Purity: 98.02%
- CAS No.: 3099808-68-8
- 화학식: C32H31ClFNO7S
- 분자량:628.11
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
GJ19 (48 h) demonstrates the highest PD-L1 inhibitory effects with an IC50 of 32.06 nM in the HTRF assay, which is better than the positive control BMS-202 (HY-19745) (IC50 = 62.1 nM)[1].
GJ19 (0.1-10 μM) binds to human/murine PD-L1 protein nicely, with KD values of 171 and 290 nM, respectively[1].
GJ19 (48 h) exhibits no/little cytotoxicity against the tested tumor cells (murine/human melanoma cell lines B16-F10/A375 human liver cancer cell line HepG2, and human breast cells MDA-MB-23l and Jurkat T cells) and exerts toxicity only upon co-culture with T cells[1].
GJ19 (12.3-1000 nM, 24 h) dose-dependently and significantly increases the mortality of HepG2 cells in the HepG2/Jurkat T cell co-culture system, and the mortality rate of HepG2 cells is higher than that of the positive control BMS-202 at a concentration of 1000 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 weeks male C57BL/6 mice were inoculated with B16-F10 cells into the right armpit (2.5×105)[1]
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Dosage:5, 15 mg/kg
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Administration:i.p.
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Result:Reduced both the tumor weights without affecting the body weight of mice.
Increased the percentages of CD3+ CD4+ cells (helper T cells) and CD3+ CD8+ cells (activated cytotoxic T cells) in melanoma tumors.
Decreased PD-L1 levels in the tumor.
Showed no abnormalities in the weight of major organs (heart, liver, and kidney).
Chemical Information
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CAS No. 3099808-68-8
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Appearance Solid
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분자량 628.11
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화학식 C32H31ClFNO7S
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Color White to off-white
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SMILES
C[C@H](O)[C@H](C(O)=O)NCC1=CC(Cl)=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)C=C1OCC4=CC=C(S(=O)(F)=O)C=C4
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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 (159.21 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 (3.98 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 (3.98 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 | 1.5921 mL | 7.9604 mL | 15.9208 mL | 39.8019 mL |
| 5 mM | 0.3184 mL | 1.5921 mL | 3.1842 mL | 7.9604 mL | |
| 10 mM | 0.1592 mL | 0.7960 mL | 1.5921 mL | 3.9802 mL | |
| 15 mM | 0.1061 mL | 0.5307 mL | 1.0614 mL | 2.6535 mL | |
| 20 mM | 0.0796 mL | 0.3980 mL | 0.7960 mL | 1.9901 mL | |
| 25 mM | 0.0637 mL | 0.3184 mL | 0.6368 mL | 1.5921 mL | |
| 30 mM | 0.0531 mL | 0.2653 mL | 0.5307 mL | 1.3267 mL | |
| 40 mM | 0.0398 mL | 0.1990 mL | 0.3980 mL | 0.9950 mL | |
| 50 mM | 0.0318 mL | 0.1592 mL | 0.3184 mL | 0.7960 mL | |
| 60 mM | 0.0265 mL | 0.1327 mL | 0.2653 mL | 0.6634 mL | |
| 80 mM | 0.0199 mL | 0.0995 mL | 0.1990 mL | 0.4975 mL | |
| 100 mM | 0.0159 mL | 0.0796 mL | 0.1592 mL | 0.3980 mL |
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