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CAY10626

Names

[ CAS No. ]:
1202884-94-3

[ Name ]:
CAY10626

[Synonym ]:
Benzamide, N-[2-(dimethylamino)ethyl]-N-methyl-4-[[[[4-[4-(4-morpholinyl)-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]phenyl]amino]carbonyl]amino]-
N-[2-(Dimethylamino)ethyl]-N-methyl-4-[({4-[4-(4-morpholinyl)-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]phenyl}carbamoyl)amino]benzamide

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> mTOR
Research Areas >> Cancer
Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

[Target]

PI3Kα:0.9 nM (IC50)

mTOR:0.6 nM (IC50)


[In Vitro]

PI3K-IN-22 (compound 46) inhibits the cell growth of PC3 and MDA-361 cells with IC50s of <3.0 and 13.0 nM[1].

[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 nude mouse[1]. PI3K-IN-22 (50, 25, 10 mg/kg; i.v.; once daily for 5 days weekly; 2 rounds) exhibits significant tumor regression in 50 mg/kg and no tumor regrowth until day 32, and tumor growth inhibition in 25 and 10 mg/kg 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].

[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.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C31H35F3N8O3

[ Molecular Weight ]:
624.657

[ Exact Mass ]:
624.278442

[ PSA ]:
107.86000

[ LogP ]:
2.42

[ Index of Refraction ]:
1.625

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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