ChemicalBook CAS DataBase List 1202884-94-3

1202884-94-3

Name	PI3K inhibitor
CAS	1202884-94-3
Molecular Formula	C31H35F3N8O3
MDL Number	MFCD18251469
Molecular Weight	624.66
MOL File	1202884-94-3.mol

Chemical Properties

density	1.35±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMF: 15 mg/ml; DMSO: 15 mg/ml; DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
form	A crystalline solid
pka	13.74±0.70(Predicted)
color	White to light yellow

Hazard Information

Description

The PI3Kinases are important downstream effectors of KRAS signaling. In preclinical studies, buparlisib (BKM120), a PI3K inhibitor, when combined with MEK inhibitor (PD1056309) led to significant synergistic activity in KRAS mutant NSCLC cell lines.

Uses

PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer[1].

Definition

ChEBI: CAY10626 is a member of ureas.

in vivo

PI3K-IN-22 (25 mg/kg; i.v.) suppresses phosphorylation of Akt T308, Akt S473 and S6K in MDA361 breast tumor cells up to 8 h in MDA361 tumor bearing nude mice demonstrated by biomarker studies^[1].
PI3K-IN-22 (50, 25, 10 mg/kg; i.v.; once daily for 5 days weekly; 2 rounds) shows good antitumor efficacy in MDA361 tumor xenograft nude mice model^[1].
PI3K-IN-22 (25 mg/kg; i.v.; a single dose) has a blood concentrationsat value of 1731 ng/mL at 8 h^[1].

Animal Model:	MDA361 tumor xenograft nude mice model^[1]
Dosage:	50, 25, 10 mg/kg
Administration:	i.v., once daily for 5 days weekly (2 rounds)
Result:	Exhibited significant tumor regression in 50 mg/kg and no tumor regrowth until day 32. Exhibited tumor growth inhibition in 25 and 10 mg/kg.

IC 50

PI3Kα: 0.9 nM (IC₅₀); mTOR: 0.6 nM (IC₅₀)

References

[1] Chen Z, et al. Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors. J Med Chem. 2010 Apr 22;53(8):3169-82. DOI:10.1021/jm901783v

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