Description
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
Product information
CAS Number: 1375469-38-7
Molecular Weight: 494.54
Formula: C25H30N6O5
Chemical Name: N-{8-[(2R)-2-hydroxy-3-(morpholin-4-yl)propoxy]-7-methoxy-1H,2H,3H,5H-imidazo[1,2-c]quinazolin-5-ylidene}-2-methylpyridine-3-carboxamide
Smiles: CC1=NC=CC=C1C(=O)N=C1N=C2C(OC)=C(C=CC2=C2NCCN12)OC[C@H](O)CN1CCOCC1
InChiKey: QJTLLKKDFGPDPF-ZKJNEQBOSA-N
InChi: InChI=1S/C25H30N6O5/c1-16-18(4-3-7-26-16)24(33)29-25-28-21-19(23-27-8-9-31(23)25)5-6-20(22(21)34-2)36-15-17(32)14-30-10-12-35-13-11-30/h3-7,17,27,32H,8-15H2,1-2H3/b29-25+/t17-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 5 mg/mL (10.11 mM; ultrasonic and adjust pH to 5 with HCl).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 has an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase. BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells.
In Vivo:
BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression.
Products are for research use only. Not for human use.
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