| ln Vitro |
In HTRF assays, GJ19 (48 h) showed the highest PD-L1 inhibitory activity with an IC50 value of 32.06 nM, which was superior to the positive control BMS-202 (IC50 = 62.1 nM) [1]. GJ19 (0.1–10 μM) bound well to human/mouse PD-L1 protein with KD values of 171 nM and 290 nM, respectively [1]. GJ19 (48 h) showed almost no cytotoxicity to the tested tumor cells (mouse/human melanoma cell line B16-F10/A375, human hepatocellular carcinoma cell line HepG2, human breast cancer cell line MDA-MB-23l, and Jurkat T cells), and only showed cytotoxicity when co-cultured with T cells [1]. GJ19 (12.3-1000 nM, 24 hours) significantly increased the mortality rate of HepG2 cells in the HepG2/Jurkat T cell co-culture system in a dose-dependent manner, and at a concentration of 1000 nM, the mortality rate of HepG2 cells was higher than that of the positive control BMS-202[1].
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|---|---|
| ln Vivo |
GJ19 (5-15 mg/kg, intraperitoneal injection) showed strong antitumor efficacy in the B16-F10 melanoma mouse model, with a TGI of 56.8% at a dose of 15 mg/kg[1].
|
| Animal Protocol |
Animal/Disease Models:6-8 week old male C57BL/6 mice were inoculated with B16-F10 cells (2.5 × 10⁵) in the right axilla [1]
Doses: 5, 15 mg/kg Route of Administration:Intraperitoneal injection Experimental Results:Tumor weight was reduced without affecting mouse body weight. The proportion of CD3⁺CD4⁺ cells (helper T cells) and CD3⁺CD8⁺ cells (activated cytotoxic T cells) in melanoma tumors was increased. The expression level of PD-L1 in tumors was reduced. No abnormalities were observed in the weight of major organs (heart, liver, and kidneys). |
| References |
| CAS # |
3099808-68-8
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|---|---|
| Appearance |
White to off-white solid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~159.21 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.98 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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