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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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ

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