Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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Targets |
IC50: 2.7 nM (PD-1/PD-L1)[1].
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ln Vitro |
Compound B2, PD-1/PD-L1-IN-10, even at low concentrations of 1 nM, significantly increases interferongamma secretion in vitro in a dose-dependent manner[1]. The viability of LLC cells and lymph node T-cells is unaffected by PD-1/PD-L1-IN-10 (compound B2)[1]. Compound B2, 0-100 nM, PD-1/PD-L1-IN-10, stabilizes the PD-L1 protein in mouse Lewis lung carcinoma (LLC) cells. Specifically, at 58 °C, compound B2, PD-1/PD-L1-IN-10, sustains the PD-L1 stability in a dose-dependent manner. suggesting that compound B2, PD-1/PD-L1-IN-10, may bind to the PD-L1 protein directly after entering LLC cells[1].
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ln Vivo |
PD-1/PD-L1-IN-10 (compound B2, 5 mg/kg, intragastric gavage) in an LLC-bearing allograft mice model demonstrates strong in vivo anticancer activity. In LLC tumor tissues, PD-1/PD-L1-IN-10 (compound B2) efficiently inhibits tumor cell proliferation and triggers apoptosis.
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Animal Protocol |
Animal/Disease Models: LLC tumor-bearing mice[1].
Doses: 2, 5 mg/kg. Route of Administration: ig, qd., for 21 days Experimental Results: Dramatically suppressed the growth of the tumor in a dose-dependent manner compared with the vehicle group. |
References |
[1]. Yiqiang OuYang, et al. Design, Synthesis, and Evaluation of o-(Biphenyl-3-ylmethoxy)nitrophenyl Derivatives as PD-1/PD-L1 Inhibitors with Potent Anticancer Efficacy In Vivo. J Med Chem. 2021 May 26.
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Molecular Formula |
C33H31N3O7
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Molecular Weight |
581.62
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CAS # |
2487550-41-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O(CC1C=CC=C(C2C=CC=CC=2)C=1C)C1=CC(=C(C=C1[N+](=O)[O-])CN[C@H](C(=O)O)C(C)O)OCC1C=CC=C(C#N)C=1
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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)
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Solubility (In Vitro) |
DMSO : 100 mg/mL (171.93 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.30 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 can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7193 mL | 8.5967 mL | 17.1934 mL | |
5 mM | 0.3439 mL | 1.7193 mL | 3.4387 mL | |
10 mM | 0.1719 mL | 0.8597 mL | 1.7193 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.