BAY-1082439 free base · Synonyms: BAY 1082439 · BAY1082439

BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor.

For research use only. Not for human or veterinary use.

Target PI3K Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

BAY-1082439 structure

CAS No.: 1375469-38-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 560.00	BP-02130-250mg	In stock	Get quote
500 mg	USD 920.00	BP-02130-500mg	In stock	Get quote
1 g	USD 1,480.00	BP-02130-1g	In stock	Get quote
2 g	USD 2,360.00	BP-02130-2g	In stock	Get quote

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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 .

Biological activity

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.

Identifiers

SMILES: COC1=C(OC[C@H](O)CN2CCOCC2)C=CC2=C1N=C(NC(=O)C1=CC=CN=C1C)N1CCN=C21
InChIKey: JGNRMIWLBBNSMU-QGZVFWFLSA-N

Specifications

MW (average): 494.5429
Formula: C₂₅H₃₀N₆O₅
CAS No.: 1375469-38-7
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1].Ningshu Liu, et al. Abstract 2799: BAY 1082439, a highly selective and balanced PI3Kα/β inhibitor demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN. Abstract nr 2799. doi:1538-7445.AM2012-2799.

[2].Yongkang Zou, et al. Co-Targeting the Cell Intrinsic and Microenvironment Pathways of Prostate Cancer by PI3Kα/β/δ inhibitor BAY1082439. Mol Cancer Ther. 2018 Oct;17(10):2091-2099.

Same target

Search PI3K

Same research area

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