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Duvelisib (IPI-145, INK1197)

Names

[ CAS No. ]:
1201438-56-3

[ Name ]:
Duvelisib (IPI-145, INK1197)

[Synonym ]:
8-Chloro-2-phenyl-3-[(1S)-1-(3H-purin-6-ylamino)ethyl]-1(2H)-isoquinolinone
IPI-145
1(2H)-Isoquinolinone, 8-chloro-2-phenyl-3-[(1S)-1-(9H-purin-6-ylamino)ethyl]-
UNII-610V23S0JI
INK1197
INK-1197
duvelisib

Biological Activity

[Description]:

Duvelisib is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.

[Related Catalog]:

Research Areas >> Cancer

[Target]

p110δ:2.5 nM (IC50)

p110γ:27.4 nM (IC50)

p110β:85 nM (IC50)

p110α:1602 nM (IC50)


[In Vitro]

PI3Kδ and PI3Kγ inhibition with IPI-145 has anti-proliferative activity in primary AML cells by inhibiting the activity of AKT and MAPK. Pre-treatment of AML cells with IPI-145 inhibits both adhesion and migration of AML blasts to bone marrow stromal cells[1]. 

[References]

[1]. Pillinger G, et al. Targeting PI3Kδ and PI3Kγ signalling disrupts human AML survival and bone marrow stromal cell mediated protection. Oncotarget. 2016 Jun 28;7(26):39784-39795.

[2]. G?ckeritz E, et al. Efficacy of phosphatidylinositol-3 kinase inhibitors with diverse isoform selectivity profiles for inhibiting the survival of chronic lymphocytic leukemia cells. Int J Cancer. 2015 Nov 1;137(9):2234-42.


[Related Small Molecules]

3-Methyladenine | LY294002 | Wortmannin | Alpelisib (BYL719) | BKM120 | Eganelisib(IPI-549) | BAY 80-6946 (Copanlisib) | Idelalisib (CAL-101) | Dactolisib (BEZ235) | Quercetin | SAR-405 | GDC-0941 | 740 Y-P | LY3023414 | 1,3-Dicaffeoylquinic acid

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C22H17ClN6O

[ Molecular Weight ]:
416.863

[ Exact Mass ]:
416.115234

[ PSA ]:
88.49000

[ LogP ]:
4.60

[ Index of Refraction ]:
1.757

[ Storage condition ]:
-20°C

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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