Home Angiogenesis PI3K inhibitor Duvelisib (IPI-145) For research use only.

Duvelisib (IPI-145)

Synonyms: INK1197

Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3.

Duvelisib (IPI-145) Chemical Structure

Duvelisib (IPI-145) Chemical Structure

CAS: 1201438-56-3

Selleck's Duvelisib (IPI-145) has been cited by 46 publications

Purity & Quality Control

Batch: Purity: 99.96%
99.96

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat Proliferation assay 3 days Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay, IC50=1.9 Μm 27774127
MOLT4 Proliferation assay 3 days Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay, IC50=2.3 μM 27774127
MV4-11 Proliferation assay 3 days Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay, IC50=4.4 μM 27774127
MOLM14 Proliferation assay 3 days Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay, IC50=1.2 μM 27774127
Loucy Proliferation assay 3 days Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay, IC50=0.98 μM 27774127
JURKAT Function assay 0.1, 1.0, and 9.0 μM IPI145 was able to inhibit Akt and S6 phosphorylation and modestly affected growth in JURKAT 30970263
MOLT3 Function assay 0.1, 1.0, and 9.0 μM IPI145 was able to inhibit Akt and S6 phosphorylation but barely affected the growth of MOLT3 T-ALL 30970263
Raji32 Function assay 1 μM effectively impaired the phosphorylation of Akt 30584254
Ramos460 Function assay 1 μM effectively impaired the phosphorylation of Akt 30584254
HBL-1 Growth inhibition assay GI50=5.3 μM 30067771
OCI-Ly3 Growth inhibition assay GI50=3.7 μM 30067771
TMD-8 Growth inhibition assay GI50=0.0005 μM 30067771
U-2932 Growth inhibition assay GI50=1.8 μM 30067771
Farage Growth inhibition assay GI50=0.04 μM 30067771
SU-DHL-10 Growth inhibition assay GI50=2.4 μM 30067771
SU-DHL-4 Growth inhibition assay GI50=0.2 μM 30067771
Karpas-422 Growth inhibition assay GI50=0.1 μM 30067771
DOHH-2 Growth inhibition assay GI50=0.05 μM 30067771
WSU-NHL Growth inhibition assay GI50=0.008 μM 30067771
Jeko-1 Growth inhibition assay GI50=1.3 μM 30067771
Mino Growth inhibition assay GI50=3.4 μM 30067771
NCI-H929 Growth inhibition assay GI50=1 μM 30067771
HH Growth inhibition assay GI50=0.01 μM 30067771
BJAB Cell viability assay 0.1, 1, 5 μM 48 and 72 h inhibited cell growth 29522278
LCL Cell viability assay 0.1, 1, 5 μM 48 and 72 h inhibited cell growth 29522278
insect cells Function assay 5 mins Inhibition of recombinant human C-terminal His6-tagged p110gamma expressed in insect cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by thin layer chromatographic method, IC50 = 0.1 μM. ChEMBL
Sf21 Function assay 5 mins Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length p85alpha expressed in baculovirus infected Sf21 cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by thin l, IC50 = 0.1 μM. ChEMBL
splenic B Antiproliferative assay 30 mins Antiproliferative activity against Balb/c mouse splenic B cells preincubated for 30 mins followed by LPS or F(ab')2 donkey anti-mouse IgM and recombinant mouse IL4 stimulation measured after 72 hrs by Alamar Blue reduction assay, EC50 = 0.1 μM. ChEMBL
Sf21 Function assay 5 mins Inhibition of N-terminal His6-tagged recombinant full-length human p110beta/untagged recombinant full length p85alpha expressed in baculovirus infected Sf21 cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by thin la, IC50 = 1 μM. ChEMBL
Sf21 Function assay 5 mins Inhibition of N-terminal His6-tagged recombinant full-length human p110alpha/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by , IC50 = 10 μM. ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3.
Targets
PI3Kδ [1]
(Cell-free assay)		 PI3Kβ [1]
(Cell-free assay)		 PI3Kγ [1]
(Cell-free assay)
23 pM(Ki) 1564 pM(Ki) 243 pM(Ki)
In vitro
In vitro

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. [1]
Cell Research Cell lines AML cell lines
Concentrations 10 μM
Incubation Time 72 h
Method

AML cell lines were treated with 10 μM IPI-145 and cultured for 72 hours.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT / p-MAPK / MAPK PI3Kγ / PI3Kδ 27174919
In Vivo
In vivo

IPI-145 (10 mg/kg, p.o.) shows well pharmacokinetics with Cmax and AUC of 390 ng/mL and 137 ng•h/mL in mouse and rat. IPI-145 (10 mg/kg) is active in murine DTH model with ~50% ear swelling. IPI-145 (10 mg/kg) demonstrates dose-dependent effect in rat collagen induced arthritis (CIA) model. IPI-145 prevents inflammation and protects joint bone and cartilage in the rat CIA model. IPI-145 (10 mg/kg,QD) demonstrates activity in rat adjuvant induced polyarthritis model. [1]
Animal Research Animal Models Brown Norway rats
Dosages (0.1, 0.3, 1, or 10 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02307461 Completed Healthy SecuraBio November 2014 Phase 1
NCT02095587 Completed Hepatic Impairment SecuraBio March 2014 Phase 1
NCT01947777 Completed Healthy SecuraBio October 2013 Phase 1
NCT01925911 Completed Healthy SecuraBio August 2013 Phase 1
NCT01836861 Completed Healthy SecuraBio March 2013 Phase 1
NCT01549106 Completed Healthy Volunteers SecuraBio August 2011 Phase 1

Chemical lnformation & Solubility

Molecular Weight 416.86 Formula

C22H17ClN6O
CAS No. 1201438-56-3 SDF Download Duvelisib (IPI-145) SDF
Smiles CC(C1=CC2=C(C(=CC=C2)Cl)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (199.1 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Whether IPI-145 S7028 is mixture of two chiral forms, if not, which form is it?

Answer:
S7028 IPI-145 is S form.

PI3K Signaling Pathway Map

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