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250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
Jurkat/PD-1 cells bind to ligerlimab (0.01 nM-1 nM), which prevents PD-L1 from binding to cells [2]. On cells expressing either or both checkpoint molecules, lerigerlimab can selectively engage and block PD-1 and CTLA-4 (EC50: 0.42 nM for PD-1+ cells and 4.8 nM for CTLA-4+ cells, 0.013 nM for PD-1 and CTLA-4+ cells)[2].
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ln Vivo |
Cynomolgus monkeys treated with lerigerlimab (75 mg/kg intravenously) showed CTLA-4 blocking effects[2]. Cynomolgus monkeys can tolerate lerigerlimab (10–100 mg/kg IV, 4 weeks) with a half-life of about 7 days[2].
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Animal Protocol |
Animal/Disease Models: Cynomolgus monkeys[4]
Doses: 75 mg/kg Route of Administration: iv Experimental Results: Increased the Ki67+ T cell fraction, and demonstrated T cell expansion in the spleen. |
References |
[1]. Jason J. Luke, et al. Lorigerlimab, a bispecific PD-1×CTLA-4 DART molecule in patients (pts) with metastatic castration-resistant prostate cancer (mCRPC): A phase 1 expansion (exp) cohort. Journal of Clinical Oncology 2023 41:6_suppl, 155-155.
[2]. Berezhnoy A, et al. Development and Preliminary Clinical Activity of PD-1-Guided CTLA-4 Blocking Bispecific DART Molecule. Cell Rep Med. 2020 Dec 22;1(9):100163. [3]. Trojaniello C, Luke JJ, Ascierto PA. Therapeutic Advancements Across Clinical Stages in Melanoma, With a Focus on Targeted Immunotherapy. Front Oncol. 2021 Jun 10;11:670726. |
CAS # |
2416595-46-3
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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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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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.