Duvelisib (IPI-145)

For research use only.

Catalog No.S7028 Synonyms: INK1197

18 publications

Duvelisib (IPI-145) Chemical Structure

Molecular Weight(MW): 416.86

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 190 In stock
USD 170 In stock
USD 970 In stock
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Selleck's Duvelisib (IPI-145) has been cited by 18 publications

4 Customer Reviews

  • PI3K inhibitor IPI-145 demonstrated to be effective on ALL-SIL cells,showed an IC50 in the lower micromolar range.

    Dr. Antonino Maria Spartà from University of Bolog. Duvelisib (IPI-145) purchased from Selleck.

  • Inhibition of PI3Kγ or PI3Kδ significantly decreased the migration of JVM3 cells. JVM3 cells were cultured in medium or stimulated for 24 h with CD40L/IL-4 and then incubated with the PI3Kγ-specific inhibitor CZC24832 (2 µM), the PI3Kδ-specific inhibitor idelalisib (1 µM), dual PI3Kδ/γ inhibitor duvelisib (1 µM), or the pan-PI3K inhibitor GDC0980 (1 µM) and subjected to a transwell migration assay. DMSO served as the vehicle control for the inhibitors, while SDF1α (100 ng/ml) served as the chemoattractant (n = 7).

    Leukemia, 2018, 32(9):1958-1969. Duvelisib (IPI-145) purchased from Selleck.

  • MM1s were incubated with increasing doses of duvelisib for 4 h after which protein was extracted. Samples were then analysed for phospho-AKT and phospho-MAPK response using Western blotting. Blots were re-probed for total AKT and MAPK to confirm sample loading.

    Blood Cancer J, 2017, 7(3):e539. Duvelisib (IPI-145) purchased from Selleck.

  • (D-E) The variation of signaling pathway-related and effector proteins after PI3K selective inhibitor INK1197 (Duvelisib) treatment and c-Jun siRNA transfection.

    PLoS One, 2016, 11(12):e0169230.. Duvelisib (IPI-145) purchased from Selleck.

Purity & Quality Control

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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 NH\obJVRem:uaX\ldoF1cW:wIHHzd4F6 NIXmcm8{KGSjeYO= NFjse5FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFr1dotifCClZXzsd{Bi\nSncjCzJIRigXNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3ME2xMlkh|pyv M4jJeVI4Pzd2MUK3
MOLT4 MXTQdo9tcW[ncnH0bY9vKGG|c3H5 MmGxN{Bl[Xm| MlPPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUOEBk\WyuczDh[pRmeiB|IHThfZMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OD1{LkOg{txO M2fsN|I4Pzd2MUK3
MV4-11 MXXQdo9tcW[ncnH0bY9vKGG|c3H5 MUizJIRigXN? NYHWO2pPSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEmFNUC9OE41KM7:TR?= NXW1dFI1Ojd5N{SxNlc>
MOLM14 NGHtNmtRem:uaX\ldoF1cW:wIHHzd4F6 NHPlXlE{KGSjeYO= NYjmSVE{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTRiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEmFNUC9NU4zKM7:TR?= NILJR2EzPzd5NEGyOy=>
Loucy NVzmXFdCWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXSzJIRigXN? NFzLeppCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzveYN6KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyPUCuPVgh|ryP NYfyWFc2Ojd5N{SxNlc>
JURKAT MkjJSpVv[3Srb36gZZN{[Xl? NWnld4RQOC5zLDCxMlAtKGGwZDC5MlAh|ryP NX6wUZY5UVCLMUS1JJdieyCjYnzlJJRwKGmwaHnibZQhSWu2IHHu[EBUPiCyaH;zdIhwenmuYYTpc44h[W6mIH3v[IV{fGy7IHHm[oVkfGWmIHfyc5d1cCCrbjDKWXJMSVR? NGjN[Vk{ODl5MEK2Ny=>
MOLT3 MorDSpVv[3Srb36gZZN{[Xl? NYq1cVR7OC5zLDCxMlAtKGGwZDC5MlAh|ryP Mn;3TXBKOTR3IIfhd{Bi[mynIITvJIlvcGmkaYSgRYt1KGGwZDDTOkBxcG:|cHjvdplt[XSrb36gZpV1KGKjcnXsfUBi\m[nY4Tl[EB1cGViZ4Lve5RpKG:oIF3PUHQ{KFRvQVzM MnvVN|A6PzB{NkO=
Raji32 M1zUcmZ2dmO2aX;uJIF{e2G7 NHntelgyKM7:TR?= Mmq3[YZn\WO2aY\lcJkhcW2yYXny[YQhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MkO0N|A2QDR{NUS=
Ramos460 NV;jPYJnTnWwY4Tpc44h[XO|YYm= NUDwNJkzOSEQvF2= M{e1XIVn\mWldHn2[Yx6KGmvcHHpdoVlKHSqZTDwbI9{eGixconsZZRqd25ib3[gRYt1 Ml[wN|A2QDR{NUS=
HBL-1 MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4fkNWdKPTB;NT6zJO69VQ>? M4TVflMxODZ5N{ex
OCI-Ly3 NWXBfXpsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVSxfWt6T0l3ME2zMlch|ryP MUGzNFA3Pzd5MR?=
TMD-8 M1jlN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVjHTVUxRTBwMECwOUDPxE1? NUG5NZVqOzByNke3O|E>
U-2932 NXPKdmZZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MofCS2k2OD1zLkig{txO NYrOOWVkOzByNke3O|E>
Farage NXXWXWVNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2jo[GdKPTB;MD6wOEDPxE1? MWqzNFA3Pzd5MR?=
SU-DHL-10 NXfxdGh[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUnHTVUxRTJwNDFOwG0> NGHmcYw{ODB4N{e3NS=>
SU-DHL-4 M1jBcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGS5WZFIUTVyPUCuNkDPxE1? M123PVMxODZ5N{ex
Karpas-422 NVPnUGVxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkLtS2k2OD1yLkGg{txO MnPZN|AxPjd5N{G=
DOHH-2 NUWyU2w6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVTHTVUxRTBwMEWg{txO Mkm2N|AxPjd5N{G=
WSU-NHL MlXvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3eycWdKPTB;MD6wNFgh|ryP NH3INFI{ODB4N{e3NS=>
Jeko-1 NYnFbo85T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWnHTVUxRTFwMzFOwG0> MnHVN|AxPjd5N{G=
Mino MkXGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIDxdoxIUTVyPUOuOEDPxE1? NFizS3g{ODB4N{e3NS=>
NCI-H929 M1LzOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXHTSFdzT0l3ME2xJO69VQ>? M4LiWlMxODZ5N{ex
HH M2HwR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mlm3S2k2OD1yLkCxJO69VQ>? M{nUO|MxODZ5N{ex
BJAB M4[2bGNmdGxidnnhZoltcXS7IHHzd4F6 M1;wZ|AvOSxiMTygOUDPxE1? NXW1fIN6PDhiYX7kJFczKGh? NXP4SXNrcW6qaXLpeIVlKGOnbHyg[5Jwf3Sq MYKyPVUzOjJ5OB?=
LCL NX73eHhwS2WubDD2bYFjcWyrdImgZZN{[Xl? M2LwWlAvOSxiMTygOUDPxE1? MoexOFgh[W6mIEeyJIg> MWrpcohq[mm2ZXSgZ4VtdCCpcn;3eIg> NFn2cnozQTV{MkK3PC=>

... 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(NC1=NC=NC2=C1N=C[NH]2)C3=CC4=CC=CC(=C4C(=O)N3C5=CC=CC=C5)Cl

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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

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.

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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