Duvelisib (IPI-145, INK1197)

Catalog No.S7028

Duvelisib (IPI-145, INK1197) 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  
In DMSO USD 190 In stock
USD 170 In stock
USD 970 In stock
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Cited by 11 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, INK1197) 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, INK1197) 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, INK1197) 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, INK1197) purchased from Selleck.

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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 NX3GO25TWHKxbHnm[ZJifGmxbjDhd5NigQ>? NH7Zb4E{KGSjeYO= M4LBR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSoXyb4F1KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyPUGuPUDPpG1? NILqfJozPzd5NEGyOy=>
MOLT4 NFi2VoVRem:uaX\ldoF1cW:wIHHzd4F6 NXfIUXg2OyCmYYnz NWX3dlhMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{Bi\nSncjCzJIRigXNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3ME2yMlMh|ryP MmHQNlc4PzRzMke=
MV4-11 MmHaVJJwdGmoZYLheIlwdiCjc4PhfS=> MnG3N{Bl[Xm| NV3nU4Z7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEmFNUC9OE41KM7:TR?= MoHZNlc4PzRzMke=
MOLM14 NW\ZNJo6WHKxbHnm[ZJifGmxbjDhd5NigQ>? MYOzJIRigXN? NVrrTnlDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTRiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEmFNUC9NU4zKM7:TR?= NWrMO|F{Ojd5N{SxNlc>
Loucy M1G3N3Bzd2yrZnXyZZRqd25iYYPzZZk> Ml7tN{Bl[Xm| M{XYTGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTH;1Z5kh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTB;MD65PEDPxE1? M2Gz[lI4Pzd2MUK3
JURKAT MoDXSpVv[3Srb36gZZN{[Xl? NUWzU3NEOC5zLDCxMlAtKGGwZDC5MlAh|ryP MlvETXBKOTR3IIfhd{Bi[mynIITvJIlvcGmkaYSgRYt1KGGwZDDTOkBxcG:|cHjvdplt[XSrb36gZY5lKG2xZHXzeIx6KGGoZnXjeIVlKGe{b4f0bEBqdiCMVWLLRXQ> NHL0WHY{ODl5MEK2Ny=>
MOLT3 MnraSpVv[3Srb36gZZN{[Xl? M333XFAvOSxiMT6wMEBidmRiOT6wJO69VQ>? NVT4XJExUVCLMUS1JJdieyCjYnzlJJRwKGmwaHnibZQhSWu2IHHu[EBUPiCyaH;zdIhwenmuYYTpc44h[nW2IHLhdoVtgSCjZn\lZ5Rm\CC2aHWg[5Jwf3SqIH;mJG1QVFR|IGStRWxN Mnu5N|A6PzB{NkO=
Raji32 NH3vc|VHfW6ldHnvckBie3OjeR?= MlK1NUDPxE1? M1fsPIVn\mWldHn2[Yx6KGmvcHHpdoVlKHSqZTDwbI9{eGixconsZZRqd25ib3[gRYt1 NFTEU4U{ODV6NEK1OC=>
Ramos460 Ml;wSpVv[3Srb36gZZN{[Xl? MlPWNUDPxE1? NFXMb4Rm\m[nY4TpeoVtgSCrbYDhbZJm\CC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? MUKzNFU5PDJ3NB?=
HBL-1 NEHWdolIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUPHTVUxRTVwMzFOwG0> NHH2fpA{ODB4N{e3NS=>
OCI-Ly3 MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NILQcVRIUTVyPUOuO{DPxE1? NXfKdHd[OzByNke3O|E>
TMD-8 M3;Pbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3;hb2dKPTB;MD6wNFA2KM7:TR?= NUnDZYs4OzByNke3O|E>
U-2932 NVHEfFV5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{D6V2dKPTB;MT64JO69VQ>? M3fJPVMxODZ5N{ex
Farage M3\tXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml3KS2k2OD1yLkC0JO69VQ>? MXuzNFA3Pzd5MR?=
SU-DHL-10 M{nNVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml3pS2k2OD1{LkSg{txO MlnzN|AxPjd5N{G=
SU-DHL-4 MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3P6[WdKPTB;MD6yJO69VQ>? Mn;ON|AxPjd5N{G=
Karpas-422 MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF7sZpNIUTVyPUCuNUDPxE1? NET4Vpk{ODB4N{e3NS=>
DOHH-2 MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGPyd2NIUTVyPUCuNFUh|ryP NUXJdYg4OzByNke3O|E>
WSU-NHL NVvCXnR3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEntZpRIUTVyPUCuNFA5KM7:TR?= NInNUGg{ODB4N{e3NS=>
Jeko-1 MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NED2RpRIUTVyPUGuN{DPxE1? NV7N[WRsOzByNke3O|E>
Mino NYD4cnBKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV;HTVUxRTNwNDFOwG0> Mmj4N|AxPjd5N{G=
NCI-H929 NXTaXWVDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mm\JS2k2OD1zIN88US=> NV30fYtkOzByNke3O|E>
HH NYHHd3JvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MknKS2k2OD1yLkCxJO69VQ>? NHfRUXA{ODB4N{e3NS=>
BJAB MW\D[YxtKH[rYXLpcIl1gSCjc4PhfS=> NU\tOFA1OC5zLDCxMEA2KM7:TR?= MmX1OFgh[W6mIEeyJIg> M2LjeYlvcGmkaYTl[EBk\WyuIHfyc5d1cA>? NWTmWnd7Ojl3MkKyO|g>
LCL MlPDR4VtdCC4aXHibYxqfHliYYPzZZk> MonsNE4yNCBzLDC1JO69VQ>? MXu0PEBidmRiN{KgbC=> NInMToVqdmirYnn0[YQh[2WubDDndo94fGh? Moe2Nlk2OjJ{N{i=

... 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 N/A

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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