Duvelisib (IPI-145, INK1197)

Catalog No.S7028

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.

Price Stock Quantity  
USD 190 In stock
USD 170 In stock
USD 970 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Duvelisib (IPI-145, INK1197) Chemical Structure

Duvelisib (IPI-145, INK1197) Chemical Structure
Molecular Weight: 416.86

Validation & Quality Control

Customer Product Validation(1)

Quality Control & MSDS

PI3K Inhibitors with Unique Features

  • Selective PI3K Inhibitors

    CAL-101 (Idelalisib, GS-1101) p110δ-selective, IC50=2.5 nM. TGX-221 p110β-specific, IC50=5 nM.

  • FDA-approved PI3K Inhibitor

    CAL-101 (Idelalisib, GS-1101) Approved by FDA for Relapsed Chronic Lymphocytic Leukemia, Follicular Lymphoma and Small Lymphocytic Lymphoma.

  • Newest PI3K Inhibitor

    VS-5584 (SB2343) Potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.

  • Classic PI3K Inhibitor

    LY294002 The first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.

Product Information

  • Compare PI3K
    Compare PI3K Products
  • Research Area
  • Inhibition Profile

Product Description

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)
PI3Kγ [1]
(Cell-free assay)
PI3Kδ [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)

 View  More

IC50 23 pM(Ki) 243 pM(Ki) 23 pM(Ki) 1564 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]
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]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Vito Palombella, Targeting PI3K- δ and PI3K-γ in Inflammation, 2012.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-29)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02292225 Recruiting Lymphocytic Leukemia, Chronic|Lymphoma, Small Lymphocytic Infinity Pharmaceuticals, Inc. February 2015 Phase 1
NCT02391545 Recruiting CD20+ Follicular Lymphoma Infinity Pharmaceuticals, Inc. December 2014 Phase 1|Phase 2
NCT02307461 Completed Healthy Infinity Pharmaceuticals, Inc. November 2014 Phase 1
NCT02204982 Active, not recruiting Follicular Lymphoma Infinity Pharmaceuticals, Inc. September 2014 Phase 3
NCT02158091 Recruiting Chronic Lymphocytic Leukemia Dana-Farber Cancer Institute|Infinity Pharmaceuticals, Inc. July 2014 Phase 1|Phase 2

view more

Chemical Information

Download Duvelisib (IPI-145, INK1197) SDF
Molecular Weight (MW) 416.86
Formula

C22H17ClN6O

CAS No. 1201438-56-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 83 mg/mL (199.1 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 1(2H)-Isoquinolinone, 8-chloro-2-phenyl-3-[(1S)-1-(9H-purin-6-ylamino)ethyl]-

Customer Product Validation (1)


Click to enlarge
Rating
Source Dr. Antonino Maria Spartà from University of Bolog. Duvelisib (IPI-145, INK1197) purchased from Selleck
Method MTT
Cell Lines ALL-SIL cells
Concentrations
Incubation Time 48 h
Results PI3K inhibitor IPI-145 demonstrated to be effective on ALL-SIL cells,showed an IC50 in the lower micromolar range.

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related PI3K Products

  • GDC-0032

    GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

    Features:A beta isoform-sparing PI3K inhibitor.

  • Pilaralisib (XL147)

    Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.

  • GNE-317

    GNE-317 is a potent, brain-penetrant PI3K inhibitor.

  • LY294002

    LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation.

  • CAL-101 (Idelalisib, GS-1101)

    CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

  • Wortmannin

    Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.

  • BEZ235 (NVP-BEZ235, Dactolisib)

    BEZ235 (NVP-BEZ235, Dactolisib) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.

  • BKM120 (NVP-BKM120, Buparlisib)

    BKM120 (NVP-BKM120, Buparlisib) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.

  • Pictilisib (GDC-0941)

    Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2.

Recently Viewed Items

Tags: buy Duvelisib (IPI-145, INK1197) | Duvelisib (IPI-145, INK1197) supplier | purchase Duvelisib (IPI-145, INK1197) | Duvelisib (IPI-145, INK1197) cost | Duvelisib (IPI-145, INK1197) manufacturer | order Duvelisib (IPI-145, INK1197) | Duvelisib (IPI-145, INK1197) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us