| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| Targets |
p110δ (IC50 = 2.5 nM); p110γ (IC50 = 27.4 nM); p110β (IC50 = 85 nM); p110α (IC50 = 1602 nM)
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|---|---|
| ln Vitro |
IPI-145 inhibits human T-cell proliferation with an EC50 of 9.5 nM and suppresses murine/human B-cell proliferation with an EC50 of 0.5 nM/0.5 nM.[1]
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| ln Vivo |
IPI-145 (10 mg/kg, p.o.) exhibits good pharmacokinetics in mice and rats, with Cmax and AUC values of 390 ng/mL and 137 ng•h/mL, respectively. With a 50% ear swelling in the murine DTH model, IPI-145 (10 mg/kg) is effective. In a rat collagen-induced arthritis (CIA) model, IPI-145 (10 mg/kg) exhibits a dose-dependent effect. In the rat CIA model, IPI-145 reduces inflammation and safeguards joint bone and cartilage. In a model of adjuvant-induced polyarthritis in rats, IPI-145 (10 mg/kg,QD) exhibits activity. [1]
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| Enzyme Assay |
Duvelisib is a selectivitep100δinhibitor with IC50of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.PI3Kδ and PI3Kγ inhibition with IPI-145 has anti-proliferative activity in primary AML cells by inhibiting the activity of AKT and MAPK. Pre-treatment of AML cells with IPI-145 inhibits both adhesion and migration of AML blasts to bone marrow stromal cells.
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| Cell Assay |
IPI-145 (10 μM) was applied to AML cell lines, and the cells were then cultured for 72 hours.
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| Animal Protocol |
Brown Norway rats
(0.1, 0.3, 1, or 10 mg/kg p.o. |
| References |
| Molecular Formula |
C22H17CLN6O
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|---|---|
| Molecular Weight |
416.86
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| Exact Mass |
416.11524
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| Elemental Analysis |
C, 63.39; H, 4.11; Cl, 8.50; N, 20.16; O, 3.84
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| CAS # |
1201438-56-3
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| Related CAS # |
Duvelisib (R enantiomer);1261590-48-0
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| Appearance |
white solid powder
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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-ZDUSSCGKSA-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-/m0/s1
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| Chemical Name |
(S)-3-(1-((9H-purin-6-yl)amino)ethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one
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| Synonyms |
IPI145; IPI 145; IPI-145; INK1197; INK 1197; INK-1197; Duvelisib; trade name: Copiktra
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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) |
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|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.00 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 (6.00 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. View More
Solubility in Formulation 3: 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03961672 | Active Recruiting |
Drug: Duvelisib | Recurrent Chronic Lymphocytic Leukemia Recurrent Small Lymphocytic Lymphoma |
City of Hope Medical Center | May 13, 2020 | Phase 2 |
| NCT03892044 | Active Recruiting |
Drug: Duvelisib Biological: Nivolumab |
Richter Syndrome Small Lymphocytic Lymphoma |
November 5, 2019 | May 13, 2020 | Phase 1 |
| NCT02783625 | Active Recruiting |
Drug: duvelisib Drug: Bortezomib |
Relapsed/Refractory T-cell Lymphomas Lymphoma |
Memorial Sloan Kettering Cancer Center |
May 2016 | Phase 1 |
| NCT03372057 | Active Recruiting |
Drug: Duvelisib | Peripheral T-cell Lymphoma | SecuraBio | February 22, 2018 | Phase 2 |
| NCT02158091 | Active Recruiting |
Drug: IPI-145 Drug: Fludarabine |
Chronic Lymphocytic Leukemia | Dana-Farber Cancer Institute | June 27, 2014 | Phase 1 Phase 2 |
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Targeting PI3K inhibits AML survival in AML cell lines and primary AML blasts. |
IPI-145 inhibits AKT phosphorylation in AML. Oncotarget. 2016 Jun 28;7(26):39784-39795. |
IPI-145 inhibits adhesion of AML blasts to primary BMSC. Oncotarget. 2016 Jun 28;7(26):39784-39795. |
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