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| ln Vitro |
Lck Inhibitor (compound 25) inhibits the T cell current sensor IL-2 death test (T-cell current, IC50 = 0.53 μM) in the same human T cells and exhibits good efficacy in the T cell current sensor IL-2 death assay (IL-2, IC50 = 0.46 μM). Comparing Lck Inhibitor to other in vitro cell assays employing blocked human cells, the inhibitory effect on the human mixed solution reaction (huMLR) is improved by a factor of ten. Lck Inhibitor also prevents biochemical cell tests and human cell mixed reaction assays from phosphorylating the TCR chain in a Lck-dependent manner. When IL-2 was stimulated using lysate and a calcium ionophore (PMA/iono) in a non-dependent manner, the efficacy of Lck Inhibitor was reduced tenfold. When the human T cell line Jurkat (JKT) was used in a general proliferation assay, Lck Inhibitor showed comparable levels of activity [1].
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| ln Vivo |
From day 9 to day 17, lick mold (0–60 mg/kg; sidewall once daily) exhibits dose-dependent suppression of arthritis [1]. Following treatment with Lck mold (sidewall 5 mg/kg), the Cmax, AUC0-∞, tmax, and F% were, in that order, 82 ng/mL, 862 ng h/mL, and 17% [1].
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| Animal Protocol |
Animal/Disease Models: Male Lewis rat (adjuvant-induced arthritis model) [1]
Doses: 0, 30 and 60 mg/kg Route of Administration: Po; one time/day; from day 9 to today 17 Experimental Results: demonstrated protection against arthritis Dose-dependent inhibition, with an estimated ED50 of 24 mg/kg. Animal/Disease Models: SD (SD (Sprague-Dawley)) rat[1] Doses: Po (pharmacokinetic/PK/PK analysis) Route of Administration: 5 mg/kg Experimental Results: Cmax, AUC0-∞, tmax and F% were 82 ng/mL, 862 ng h respectively /mL and 17%, respectively. |
| References |
[1]. Martin, Matthew W.; Newcomb, John; Nunes, Joseph J.; et al. Structure-Based Design of Novel 2-Amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as Potent and Orally Active Inhibitors of Lymphocyte Specific Kinase (Lck): Synthesis, SAR, and In Vivo Anti-Inflammatory Activity. Journal of Medicinal Chemistry (2008), 51(6), 1637-1648.
[2]. Liew, Chin Y.; Ma, Xiao H.; Liu, Xianghui; Yap, Chun W. SVM Model for Virtual Screening of Lck Inhibitors. Journal of Chemical Information and Modeling (2009), 49(4), 877-885. |
| Molecular Formula |
C31H30N8O
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|---|---|
| Molecular Weight |
530.63
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| Exact Mass |
530.2543
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| CAS # |
847950-09-8
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| Related CAS # |
Lck inhibitor 2;944795-06-6
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| SMILES |
O=C1N(C2=C(C)C=CC=C2C)C3=NC4=CC=CC=C4N3C5=NC(NC6=CC=C(N7CCN(C)CC7)C=C6)=NC=C15
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| Synonyms |
TCS 7003; TC S 7003; TC-S 7003
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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 (~188.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. 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 (4.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8846 mL | 9.4228 mL | 18.8455 mL | |
| 5 mM | 0.3769 mL | 1.8846 mL | 3.7691 mL | |
| 10 mM | 0.1885 mL | 0.9423 mL | 1.8846 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.
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