BAY1082439

Name: BAY1082439
Brand: TargetMol
SKU: T14511
Rating: 4.5 (1 reviews)

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Catalog No. T14511Cas No. 1375469-38-7

BAY1082439, an orally bioavailable, selective inhibitor of PI3Kα/β/δ, demonstrates high efficacy in inhibiting the growth of Pten-null prostate cancer [1][2]. Additionally, BAY1082439 is effective against mutated forms of PIK3CA.

BAY1082439

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Catalog No. T14511Cas No. 1375469-38-7

Pack Size	Price	Availability
1 mg	$31	Backorder
2 mg	$44	Backorder
5 mg	$72	Backorder
10 mg	$122	Backorder
25 mg	$198	Backorder
50 mg	$369	Backorder
100 mg	$549	Backorder

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Product Introduction

Bioactivity

Description	BAY1082439, an orally bioavailable, selective inhibitor of PI3Kα/β/δ, demonstrates high efficacy in inhibiting the growth of Pten-null prostate cancer [1][2]. Additionally, BAY1082439 is effective against mutated forms of PIK3CA.
In vitro	BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells[2]. BAY1082439 exhibits an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM) and shows >1000-fold selectivity against mTOR kinase[1].
In vivo	BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) effectively prevents the progression of Pten-null prostate cancer[2].

Chemical Properties

Molecular Weight	494.54
Formula	C₂₅H₃₀N₆O₅
Cas No.	1375469-38-7
Smiles	COc1c(OC[C@H](O)CN2CCOCC2)ccc2C3=NCCN3C(NC(=O)c3cccnc3C)=Nc12
Relative Density.	1.43 g/cm3 (Predicted)

Storage & Solubility Information

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Solubility Information	DMSO: Slightly soluble

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

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