PI3Kδ-IN-8

PI3Kδ-IN-8 is a potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 3.3 nM. PI3Kδ-IN-8 shows selectivity for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50=377.2, 241.6, 17.9 nM, respectively) . PI3Kδ-IN-8 has anti-tumor activity[1].

Product Specifications

CAS Number

[2101518-75-4]

UNSPSC

12352005

Target

PI3K

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pi3kδ-in-8.html

Solubility

10 mM in DMSO

Smiles

N#CC1=C(N[C@H](C(C(C2=CC=C(F)C=C2)=C3C=CC(F)=CN43)=C(C5=CC=CC=C5)C4=O)C)N=C(N)N=C1N

Molecular Formula

C28H21F2N7O

Molecular Weight

509.51

References & Citations

[1]Shukla MR, et, al. Discovery of a Potent and Selective PI3Kδ Inhibitor (S) -2,4-Diamino-6- ((1- (7-fluoro-1- (4-fluorophenyl) -4-oxo-3-phenyl-4H-quinolizin-2-yl) ethyl) amino) pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models. J. Med. Chem. 2020 Dec 1.