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PIK-293 (IC87114), the parent compound of PIK-294, is a novel, potent, and the first isoform-selective PI3K (phosphatidylinositol 3-kinase) inhibitor with with potential anticancer activity. It is 500-, 100- and 50-fold less potent than PI3Kα/β/γ to inhibit PI3Kδ with an IC50 of 0.24 M.
Targets |
PI3Kδ (IC50 = 0.24 μM); PI3Kβ (IC50 = 10 μM); PI3Kγ (IC50 = 25 μM); PI3Kα (IC50 = 100 μM)
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ln Vitro |
Kinase Assay: PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively. PIK-293 inhibits the p110α, p110β, p110δ, and p110γ with IC50 of 100 μM, 25 μM, 0.24 μM,and 10 &kkkmu;M. PIK-293 is the parent compound of PIK-294. |
ln Vivo |
N/A
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Enzyme Assay |
PIK-293 is a PI3K inhibitor. With an IC50 of 0.24 μM and being 500-, 100- and 50-fold less potent than PI3Kα/β/γ, respectively. The IC50 values for PIK-293 are 100 μM, 25 μM, 0.24 μM,and 10 &kkkmu;M for the inhibition of p110α, p110β, p110δ, and p110γ. Its parent substance, PIK-293 is the parent compound of PIK-294.
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References |
Molecular Formula |
C22H19N7O
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Molecular Weight |
397.432563066483
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Exact Mass |
397.1651
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Elemental Analysis |
C, 66.49; H, 4.82; N, 24.67; O, 4.03
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CAS # |
900185-01-5
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Related CAS # |
900185-01-5
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Appearance |
Solid powder
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SMILES |
CC1=C2C(=CC=C1)N=C(N(C2=O)C3=CC=CC=C3C)CN4C5=NC=NC(=C5C=N4)N
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InChi Key |
KQDBVHKNIYROHU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H19N7O/c1-13-6-3-4-9-17(13)29-18(27-16-8-5-7-14(2)19(16)22(29)30)11-28-21-15(10-26-28)20(23)24-12-25-21/h3-10,12H,11H2,1-2H3,(H2,23,24,25)
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Chemical Name |
2-[(4-aminopyrazolo[3,4-d]pyrimidin-1-yl)methyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one
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Synonyms |
PIK293; PIK 293; PIK-293
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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)
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Solubility (In Vitro) |
DMSO: 50~80 mg/mL (125.8~201.3mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.29 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. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.15 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 12.5 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. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.15 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 | 2.5162 mL | 12.5808 mL | 25.1617 mL | |
5 mM | 0.5032 mL | 2.5162 mL | 5.0323 mL | |
10 mM | 0.2516 mL | 1.2581 mL | 2.5162 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.
(Top panel) Structure of PIK-39 bound to p110γ and predicted binding mode for IC87114, PIK-293 and PIK-294. Cell. 2006 May 19;125(4):733-47. td> |