1202884-94-3

1202884-94-3 structure

Name: CAY10626
Chemical Name: N-[2-(dimethylamino)ethyl]-N-methyl-4-[[4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)pyrrolo[2,3-d]pyrimidin-2-yl]phenyl]carbamoylamino]benzamide
CAS Number: 1202884-94-3
Molecular Formula: C₃₁H₃₅F₃N₈O₃
Molecular Weight: 624.657
Catalog: Signaling Pathways PI3K/Akt/mTOR mTOR
Create Date: 2017-10-09 13:21:15
Modify Date: 2024-01-14 18:13:25
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].

Name	N-[2-(dimethylamino)ethyl]-N-methyl-4-[[4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)pyrrolo[2,3-d]pyrimidin-2-yl]phenyl]carbamoylamino]benzamide
Synonyms	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

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.

1202885-81-1

142-25-6

1202884-94-3

Literature: Wyeth Patent: US2010/3250 A1, 2010 ; Location in patent: Page/Page column 27 ; US 20100003250 A1

Precursor 2
1202885-81-1 142-25-6
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