| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
GSK251 targets phosphoinositide 3-kinase delta (PI3Kδ). It is a highly potent and selective inhibitor of this kinase, with a unique binding mode. PI3Kδ is a key enzyme in the PI3K/AKT/mTOR signaling pathway, which is involved in cell growth, proliferation, and survival.
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|---|---|
| ln Vitro |
Specific in vitro potency values such as IC50 for GSK251 are not detailed in the available summaries. It is characterized as a highly potent and selective PI3Kδ inhibitor. Further characterization would require reference to the primary literature.
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| ln Vivo |
Specific in vivo efficacy data for GSK251 are not detailed in the available summaries. It is described as orally bioavailable, suggesting potential for in vivo efficacy in relevant disease models.
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| Enzyme Assay |
The enzymatic activity of GSK251 is assessed using kinase inhibition assays with recombinant PI3Kδ protein. Assays are performed in kinase buffer with ATP and a substrate, and IC50 values are calculated.
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| Cell Assay |
The cellular activity of GSK251 is evaluated in PI3Kδ-dependent cell lines. Cells are treated with the compound, and downstream signaling (e.g., AKT phosphorylation) is assessed by Western blot.
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| Animal Protocol |
In vivo efficacy of GSK251 would typically be evaluated in mouse models of B-cell malignancies or other PI3Kδ-driven diseases. Animals would be administered the compound orally to assess tumor growth inhibition and target modulation.
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| ADME/Pharmacokinetics |
GSK251 has a molecular formula of C29H37FN6O4S and a molecular weight of 584.71. Its IUPAC name is N-(2-(2-fluoro-4-((4-isopropylpiperazin-1-yl)methyl)phenyl)pyridin-4-yl)-2-methoxy-5-morpholinopyridine-3-sulfonamide. It is soluble in DMSO (62.5 mg/mL with ultrasonic and warming).
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for GSK251 are not available in the cited literature. The compound is intended for research use only. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
GSK251 is a highly potent, selective, orally bioavailable PI3Kδ inhibitor with a novel binding mode. It was developed by GSK and is a valuable tool for studying PI3Kδ signaling in cancer and immunology research.
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| Molecular Formula |
C29H37FN6O4S
|
|---|---|
| Molecular Weight |
584.71
|
| Exact Mass |
584.26
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| Elemental Analysis |
C, 59.57; H, 6.38; F, 3.25; N, 14.37; O, 10.94; S, 5.48
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| CAS # |
2125968-05-8
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| PubChem CID |
130302563
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
9
|
| Heavy Atom Count |
41
|
| Complexity |
912
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C)N1CCN(CC1)CC2=CC(=C(C=C2)C3=NC=CC(=C3)NS(=O)(=O)C4=C(N=CC(=C4)N5CCOCC5)OC)F
|
| InChi Key |
ODQVPYNCHSLNGV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C29H37FN6O4S/c1-21(2)35-10-8-34(9-11-35)20-22-4-5-25(26(30)16-22)27-17-23(6-7-31-27)33-41(37,38)28-18-24(19-32-29(28)39-3)36-12-14-40-15-13-36/h4-7,16-19,21H,8-15,20H2,1-3H3,(H,31,33)
|
| Chemical Name |
N-(2-(2-fluoro-4-((4-isopropylpiperazin-1-yl)methyl)phenyl)pyridin-4-yl)-2-methoxy-5-morpholinopyridine-3-sulfonamide
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| Synonyms |
GSK251; GSK 251; GSK-251;
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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)
|
| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~106.89 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.56 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 20.8 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: ≥ 2.08 mg/mL (3.56 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 20.8 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: ≥ 2.08 mg/mL (3.56 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 | 1.7102 mL | 8.5512 mL | 17.1025 mL | |
| 5 mM | 0.3420 mL | 1.7102 mL | 3.4205 mL | |
| 10 mM | 0.1710 mL | 0.8551 mL | 1.7102 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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