Duvelisib (IPI-145)

別名: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)化学構造

CAS No. 1201438-56-3

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 37000 国内在庫あり
JPY 25500 国内在庫あり
JPY 145500 国内在庫あり
JPY 598500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(47)

製品安全説明書

現在のバッチを見る: 純度: 99.96%
99.96

Duvelisib (IPI-145)関連製品

シグナル伝達経路

PI3K阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
Ramos460 Function assay 1 μM effectively impaired the phosphorylation of Akt 30584254
Raji32 Function assay 1 μM effectively impaired the phosphorylation of Akt 30584254
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
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
Loucy Proliferation assay 3 days Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay, IC50=0.98 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
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
MOLT4 Proliferation assay 3 days Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay, IC50=2.3 μM 27774127
Jurkat Proliferation assay 3 days Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay, IC50=1.9 Μm 27774127
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
OCI-Ly3 Growth inhibition assay GI50=3.7 μM 30067771
HBL-1 Growth inhibition assay GI50=5.3 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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 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]

細胞実験 細胞株 AML cell lines
濃度 10 μM
反応時間 72 h
実験の流れ

AML cell lines were treated with 10 μM IPI-145 and cultured for 72 hours.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot PI3Kγ / PI3Kδ p-AKT / AKT / p-MAPK / MAPK 29522278
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]

動物実験 動物モデル Brown Norway rats
投与量 (0.1, 0.3, 1, or 10 mg/kg
投与経路 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

化学情報

分子量 416.86 化学式

C22H17ClN6O

CAS No. 1201438-56-3 SDF Download Duvelisib (IPI-145) SDFをダウンロードする
Smiles CC(C1=CC2=C(C(=CC=C2)Cl)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
保管

In vitro
Batch:

DMSO : 83 mg/mL ( (199.1 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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よくある質問(FAQ)

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

回答
S7028 IPI-145 is S form.

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