CAY10626CAS: 1202884-94-3
MF: C31H35F3N8O3
MW: 624.7

CAY10626 (CAS 1202884-94-3)

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Synonym: 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]-benzamide
Application: CAS: 1202884-94-3, MF: C31H35F3N8O3, MW: 624.7
CAS Number: 1202884-94-3
Molecular Weight: 624.7
Molecular Formula: C31H35F3N8O3
* Refer to Certificate of Analysis for lot specific data (including water content).

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3, important second messengers that modulate the activity of downstream targets Akt and mTOR. Aberrent PI3K/Akt is associated with many human cancers. CAY10626 is a potent, dual PI3Kα/mTOR inhibitor with IC50 values of 0.9 and 0.6 nM for the two respective kinases.In a tumor cell growth inhibition assay, CAY10626 demonstrates IC50 values of <3 and 13 nM for MDA361 (breast) and PC3 (prostate) cancer cell lines, respectively. When administered at 25-50 mg/k to MD361 xenograft mice, phosphorylation of the downstream targets of PI3Kα and mTOR (Akt T308, Akt S473, and S6K) was suppressed, and significant tumor regression was observed.


References

1. Rameh, L.E., et al. 1999. J. Biol. Chem. 274: 8347-8350. PMID: 10085060
2. Chen, Z., et al. 2010. J. Med. Chem. 53: 3169-3182. PMID: 20334367

Physical State :
Solid
Solubility :
Soluble in DMSO (~15 mg/ml), DMF (~15 mg/ml), and 1:10DMSO:PBS(pH7.2) (~0.1 mg/ml).
Storage :
Store at -20° C
Boiling Point :
~646.1° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
mTOR: IC50 = 0.6 nM (human); PI3Kα: IC50 = 0.9 nM (human); MDA361: IC50 = <3 nM (human); PC3: IC50 = <13 nM (human)
pK Values :
pKa: 13.75 (Predicted), pKb: 8.38 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
44599690
MDL Number :
MFCD18251469
SMILES :
O=C(NC1=CC=C(C(N(C)CCN(C)C)=O)C=C1)NC2=CC=C(C3=NC(N4CCOCC4)=C(C=CN5CC(F)(F)F)C5=N3)C=C2

Download SDS (MSDS)

Certificate of Analysis

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