Duvelisib (IPI-145)

For research use only.

Catalog No.S7028 Synonyms: INK1197

28 publications

Duvelisib (IPI-145) Chemical Structure

CAS No. 1201438-56-3

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.

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10mM (1mL in DMSO) USD 190 In stock
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Selleck's Duvelisib (IPI-145) has been cited by 28 publications

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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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat MlK0VJJwdGmoZYLheIlwdiCjc4PhfS=> MVmzJIRigXN? MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEq3cnvheEBk\WyuczDh[pRmeiB|IHThfZMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OD1zLkmg{rxu MlKxNlc4PzRzMke=
MOLT4 NUPmSIJNWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{fMdVMh\GG7cx?= MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTGS0JINmdGy|IHHmeIVzKDNiZHH5d{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxRTJwMzFOwG0> M2TGflI4Pzd2MUK3
MV4-11 MUPQdo9tcW[ncnH0bY9vKGG|c3H5 NVjKbmJQOyCmYYnz NHvQb3NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOE0yOSClZXzsd{Bi\nSncjCzJIRigXNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3ME20MlQh|ryP NEj4d2ozPzd5NEGyOy=>
MOLM14 MnTaVJJwdGmoZYLheIlwdiCjc4PhfS=> MUCzJIRigXN? NGHaZ3RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUG0yPCClZXzsd{Bi\nSncjCzJIRigXNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3ME2xMlIh|ryP Ml;kNlc4PzRzMke=
Loucy NV\6XlkyWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFnGZ5I{KGSjeYO= NVzSNIR5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMc5VkgSClZXzsd{Bi\nSncjCzJIRigXNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3ME2wMlk5KM7:TR?= MUCyO|c4PDF{Nx?=
JURKAT NXHP[|JKTnWwY4Tpc44h[XO|YYm= MnrUNE4yNCBzLkCsJIFv\CB7LkCg{txO MmLWTXBKOTR3IIfhd{Bi[mynIITvJIlvcGmkaYSgRYt1KGGwZDDTOkBxcG:|cHjvdplt[XSrb36gZY5lKG2xZHXzeIx6KGGoZnXjeIVlKGe{b4f0bEBqdiCMVWLLRXQ> NELSVJk{ODl5MEK2Ny=>
MOLT3 NH7O[GtHfW6ldHnvckBie3OjeR?= NXfESI9LOC5zLDCxMlAtKGGwZDC5MlAh|ryP NHHuWphKWElzNEWge4F{KGGkbHWgeI8hcW6qaXLpeEBCc3RiYX7kJHM3KHCqb4PwbI9zgWyjdHnvckBjfXRiYnHy[Yx6KGGoZnXjeIVlKHSqZTDndo94fGhib3[gUW9NXDNiVD3BUGw> MmD5N|A6PzB{NkO=
Raji32 M2nUeWZ2dmO2aX;uJIF{e2G7 NY\icplmOSEQvF2= MVXl[oZm[3SrdnXsfUBqdXCjaYLl[EB1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> MYCzNFU5PDJ3NB?=
Ramos460 M1X2dGZ2dmO2aX;uJIF{e2G7 MWCxJO69VQ>? M{PpToVn\mWldHn2[Yx6KGmvcHHpdoVlKHSqZTDwbI9{eGixconsZZRqd25ib3[gRYt1 MkfMN|A2QDR{NUS=
HBL-1 M2PZOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVXkcmdTT0l3ME21MlMh|ryP NFK2e5o{ODB4N{e3NS=>
OCI-Ly3 NGjEeZJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnv3S2k2OD1|Lkeg{txO NWf1[|hsOzByNke3O|E>
TMD-8 MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVjHTVUxRTBwMECwOUDPxE1? M{K3NFMxODZ5N{ex
U-2932 NFztTo5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYLHTVUxRTFwODFOwG0> MYCzNFA3Pzd5MR?=
Farage M2Tq[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MU\HTVUxRTBwMESg{txO M4rjSlMxODZ5N{ex
SU-DHL-10 M2nqW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYPHTVUxRTJwNDFOwG0> MUWzNFA3Pzd5MR?=
SU-DHL-4 M4T4Z2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYrHTVUxRTBwMjFOwG0> NHnGdHM{ODB4N{e3NS=>
Karpas-422 MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2\sS2dKPTB;MD6xJO69VQ>? MU[zNFA3Pzd5MR?=
DOHH-2 MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX;HTVUxRTBwMEWg{txO NIHE[nY{ODB4N{e3NS=>
WSU-NHL NEXiW2hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1vrZ2dKPTB;MD6wNFgh|ryP NUTHSGlLOzByNke3O|E>
Jeko-1 Mn7RS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4foWmdKPTB;MT6zJO69VQ>? NHLuZ5Y{ODB4N{e3NS=>
Mino M1rtOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfoS2k2OD1|LkSg{txO NXfFd|VzOzByNke3O|E>
NCI-H929 MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{jHOGdKPTB;MTFOwG0> M4TXcFMxODZ5N{ex
HH MmjWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2[0eWdKPTB;MD6wNUDPxE1? Mn\WN|AxPjd5N{G=
BJAB MnraR4VtdCC4aXHibYxqfHliYYPzZZk> MkLONE4yNCBzLDC1JO69VQ>? MXO0PEBidmRiN{KgbC=> NGPvcnpqdmirYnn0[YQh[2WubDDndo94fGh? MWKyPVUzOjJ5OB?=
LCL NHjCZ3BE\WyuII\pZYJqdGm2eTDhd5NigQ>? NXO4NHVtOC5zLDCxMEA2KM7:TR?= MkfPOFgh[W6mIEeyJIg> NYDuS2FmcW6qaXLpeIVlKGOnbHyg[5Jwf3Sq NWXySlZpOjl3MkKyO|g>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-MAPK / MAPK ; 

PubMed: 27174919     


AML cell lines and primary AML blasts were treated with increasing doses of IPI-145 (nM) and cultured for 4 hours. Whole cell extracts were prepared and Western blot analysis was conducted for pAKT, pMAPK, and total AKT and MAPK protein levels.

PI3Kγ / PI3Kδ ; 

PubMed: 29522278     


Effects of duvelisib on the PI3K/Akt pathway in B and T cell lines. EBV-negative B cell lines [BJAB and Akata (-)], EBV-positive B cell lines [Akata (+), Mutu I, LCL, Raji, and P3HR1], and EBV-negative T cell line (Jurkat) were treated without (-) or with 1 or 5 μmol/L duvelisib for 48 h. Cell lysates were then immunoblotted for the indicated proteins involved in PI3K/Akt signaling.

27174919 29522278
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]

Protocol

Solubility (25°C)

In vitro DMSO 83 mg/mL (199.1 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 416.86
Formula

C22H17ClN6O

CAS No. 1201438-56-3
Storage powder
in solvent
Synonyms INK1197
Smiles CC(C1=CC2=C(C(=CC=C2)Cl)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02307461 Completed Drug: IPI-145 (duvelisib)|Drug: IPI-145 Healthy Verastem Inc. November 2014 Phase 1
NCT02095587 Completed Drug: IPI-145 Hepatic Impairment Verastem Inc. March 2014 Phase 1
NCT01947777 Completed Drug: IPI-145|Drug: Rifampin Healthy Verastem Inc. October 2013 Phase 1
NCT01925911 Completed Drug: IPI-145|Drug: Midazolam Healthy Verastem Inc. August 2013 Phase 1
NCT01836861 Completed Drug: IPI-145 Healthy Verastem Inc. March 2013 Phase 1
NCT01549106 Completed Drug: IPI-145|Drug: Placebo Healthy Volunteers Verastem Inc. August 2011 Phase 1

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID