Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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ADH-503 free base [(Z)-Leukadherin-1] is a novel, potent, selective, orally bioactive and allosteric agonist of the integrin CD11b to mitigate myeloid cell immunosuppression. The partial activation of CD11b by ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhanced dendritic cell responses. These actions, in turn, improve antitumor T cell immunity and render checkpoint inhibitors effective in previously unresponsive PDAC models.
ln Vitro |
(Z)-Leukadherin-1 (ADH-503 free base; 4 μM; 8 days) decreases the overall number of CD11b+ cells that infiltrate tumors as well as the subsets of CD11b+ monocytes, granulocytes, eosinophils, and macrophages [1].
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ln Vivo |
Z-leukadherin-1 (ADH-503 free base; orally administered; doses of 30, 60, or 120 mg/kg; administered twice daily for 60 days) slows the growth of the tumor, which reduces the number of tumors in the time point analysis burden and increases overall survival [1]. The maximal concentration of (Z)-Leukadherin-1 is 1716 and 2594 ng/ml, with a mean half-life of 4.68 and 3.95 hours (oral gavage; 30, 100 mg/kg; twice daily; days 1 and 5). 30 The AUC0-t in plasma were 6950 ng.h/ml and 13962 ng.h/ml at the mg/kg and 100 mg/kg dosages, respectively [1].
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Animal Protocol |
Animal/Disease Models: KPC mouse [p48-CRE/Lox-stop-Lox(LSL)-KrasG12D/p53flox/flox][1]
Doses: 30, 60 or 120 mg/kg Route of Administration: po (oral gavage); 60-day Experimental Results: Delays tumor progression, results in Dramatically lower tumor burden in time point analysis, and improves overall survival. Animal/Disease Models: Male rat[1] Doses: 30, 100 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: po (oral gavage), twice (two times) daily; results on days 1 and 5: 30 mg and 100 mg, the average half-lives were 4.68 and 3.95 hrs (hrs (hours)), respectively, the maximum concentrations were 1716 and 2594 ng/ml, respectively, and the AUC0-t in plasma were 6950 and 13962 ng.h/ml/kg respectively. |
References |
[1]. Panni RZ, et al. Agonism of CD11b reprograms innate immunity to sensitize pancreatic cancer to immunotherapies. Sci Transl Med. 2019 Jul 3;11(499).
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Molecular Formula |
C₂₇H₂₈N₂O₅S₂
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Molecular Weight |
524.65
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CAS # |
2055362-72-4
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Related CAS # |
Leukadherin-1;344897-95-6;ADH-503;2055362-74-6
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SMILES |
O=C([O-])C1=CC=C(C2=CC=C(/C=C(SC(N3CC4=CC=CC=C4)=S)/C3=O)O2)C=C1.OCC[N+](C)(C)C.[(Z)]
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Synonyms |
ADH-503 free base ADH-503 ADH 503 ADH503 Leukadherin-1 choline LA1
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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 : ~4.55 mg/mL (~10.80 mM)
Methanol :< 1 mg/mL |
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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.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9060 mL | 9.5302 mL | 19.0603 mL | |
5 mM | 0.3812 mL | 1.9060 mL | 3.8121 mL | |
10 mM | 0.1906 mL | 0.9530 mL | 1.9060 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.