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5mg |
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25mg |
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50mg |
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100mg |
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Purity: ≥98%
Duvelisib R enantiomer is the R-isomer of Duvelisib (formerly known as IPI-145 and INK1197, trade name: Copiktra) which is an isoquinolinone derivative and a novel potent, oral and selective small-molecule phosphoinositide-3 kinases (PI3K) inhibitor that selectively and potently inhibits two PI3K isoforms, PI3K-δ and PI3K-γ, with half maximal inhibition concentration IC50 of 2.5 nM and 27 nM respectively. FDA approved duvelisib in September 2018 to treat small lymphocytic lymphoma, follicular lymphoma, and chronic lymphocytic leukemia that has relapsed or is resistant to treatment. Despite having a preference for PI3K-δ and PI3K-γ, IPI-145 also inhibits PI3K-α and PI3K-β to a lesser extent, with IC50 values of 1602 nM and 85 nM, respectively. Phosphoinositide-3-kinase (PI3K) is an enzyme group, known to regulate key survival pathways in acute myeloid leukaemia (AML). It produces phosphatidylinositol-3,4,5-triphosphate, which offers a membrane docking site for protein kinaseB activation. There are four isoforms of the p110 catalytic subunit of PI3K:,, and. In contrast to the highly variable frequency of PI3Kγ expression, the PI3Kδ isoform is consistently expressed in AML cells. The roles of these individual catalytic enzymes have not been fully elucidated in AML, so the function of these two p110 subunits in human AML blast survival was investigated using the PI3K p110δ and p110γ targeted inhibitor IPI-145 (duvelisib) and specific p110δ and p110γ shRNA.
Targets |
PI3K
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ln Vitro |
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ln Vivo |
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Cell Assay |
IPI-145 suppresses murine/human B-cell proliferation with EC50 of 0.5 nM/0.5 nM and also inhibits human T-cell proliferation with EC50 of 9.5 nM.
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Animal Protocol |
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References |
Molecular Formula |
C22H17CLN6O
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Molecular Weight |
416.86
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CAS # |
1261590-48-0
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Related CAS # |
Duvelisib;1201438-56-3
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Appearance |
Solid
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SMILES |
C[C@H](C1=CC2=C(C(=CC=C2)Cl)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
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InChi Key |
SJVQHLPISAIATJ-CYBMUJFWSA-N
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InChi Code |
InChI=1S/C22H17ClN6O/c1-13(28-21-19-20(25-11-24-19)26-12-27-21)17-10-14-6-5-9-16(23)18(14)22(30)29(17)15-7-3-2-4-8-15/h2-13H,1H3,(H2,24,25,26,27,28)/t13-/m1/s1
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Chemical Name |
8-chloro-2-phenyl-3-[(1R)-1-(7H-purin-6-ylamino)ethyl]isoquinolin-1-one
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Synonyms |
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.00 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: ≥ 2.5 mg/mL (6.00 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. View More
Solubility in Formulation 3: ≥ 2.38 mg/mL (5.71 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. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% Propylene glycol : 30mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3989 mL | 11.9944 mL | 23.9889 mL | |
5 mM | 0.4798 mL | 2.3989 mL | 4.7978 mL | |
10 mM | 0.2399 mL | 1.1994 mL | 2.3989 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.
Targeting PI3K inhibits AML survival in AML cell lines and primary AML blasts.Oncotarget.2016 Jun 28;7(26):39784-39795. th> |
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IPI-145 inhibits AKT phosphorylation in AML.Oncotarget.2016 Jun 28;7(26):39784-39795. td> |
IPI-145 inhibits adhesion of AML blasts to primary BMSC.Oncotarget.2016 Jun 28;7(26):39784-39795. td> |