| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
pIC50: 7.5 (SYK) and 7.1 (pErk)[1]
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|---|---|
| ln Vitro |
GSK143 dihydrochloride (compound 20) inhibits the following: JAK1/2/3 (pIC50=5.8/5.8/5.7), Aurora B (pIC50=4.8), hWB (pIC50=6.6), hERG (pIC50=4.7), LCK (pIC50=5.3), LYN (pIC50=5.4), and ZAP-70 (pIC50=4.7)[1]. The CLL cells exhibit an IC50 of 323 nM with GSK 143 dihydrochloride (10–10,000 nM; every 24 hours for three days). Early signaling processes, such as SYK phosphorylation and calcium flow, are abrogated by GSK 143 dihydrochloride (1 GSK143 dihydrochloride; 0.1-10 μM; for 30 min)[2].
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| ln Vivo |
In the intestinal muscularis, GSK143 (0.1–10 mg/kg; orally; 1.5 hours) decreases inflammation and inhibits the recruitment of immune cells[3]. The cutaneous reverse passive Arthus reaction is reduced by GSK143 (3, 10, 30, 100 mg/kg; oral; one hour before ovalbumin challenge) in a dose-dependent manner by around 50% and 70% at 10 mg/kg and 30 mg/kg, respectively[2]. GSK143 in rats has a T1/2 of 4.2 hours, a low clearance of 16 mL/min/kg, a moderate bioavailability of 30%, and a Vss of 4.1 L/kg (iv of 1 mg/kg; po of 3 mg/kg)[1].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Chronic lymphocytic leukaemia (CLL) cells Tested Concentrations: 10, 100, 1000, 10000 nM Incubation Duration: Every 24 hrs (hours) for 3 days Experimental Results: Had an IC50 of 323 nM. |
| Animal Protocol |
Animal/Disease Models: Wild type C57NL/BL6 mice, 10-12 weeks old[3]
Doses: 0.1, 1, 3, 10 mg/kg Route of Administration: po (oral gavage) 1.5 hrs (hours) before Intestinal manipulation (IM) Experimental Results: diminished inflammation and prevented recruitment of immune cells in the intestinal muscularis. Animal/Disease Models: Male CD rats (175-200 g)[1] Doses: 1 mg/kg of iv; 3 mg/kg of po (pharmacokinetic/PK Analysis) Route of Administration: IV or PO Experimental Results: Had a T1/2 of 4.2 hrs (hours), low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg. |
| References |
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| Molecular Formula |
C17H23CLN6O2
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|---|---|
| Molecular Weight |
378.86
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| Exact Mass |
414.133
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| CAS # |
2341796-81-2
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| Related CAS # |
GSK143;1240390-27-5
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| PubChem CID |
138991755
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
443
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| Defined Atom Stereocenter Count |
2
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| SMILES |
N(C1C=CC(C)=CC=1)C1=NC(N[C@@H]2CCOC[C@@H]2N)=NC=C1C(=O)N.Cl
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| InChi Key |
UEHPBSLIDBDMCZ-WICJZZOFSA-N
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| InChi Code |
InChI=1S/C17H22N6O2.2ClH/c1-10-2-4-11(5-3-10)21-16-12(15(19)24)8-20-17(23-16)22-14-6-7-25-9-13(14)18;;/h2-5,8,13-14H,6-7,9,18H2,1H3,(H2,19,24)(H2,20,21,22,23);2*1H/t13-,14+;;/m0../s1
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| Chemical Name |
2-[[(3R,4R)-3-aminooxan-4-yl]amino]-4-(4-methylanilino)pyrimidine-5-carboxamide;dihydrochloride
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O : 100 mg/mL (240.78 mM)
DMSO : ≥ 50 mg/mL (120.39 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.02 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 (6.02 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6395 mL | 13.1975 mL | 26.3950 mL | |
| 5 mM | 0.5279 mL | 2.6395 mL | 5.2790 mL | |
| 10 mM | 0.2639 mL | 1.3197 mL | 2.6395 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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