BAY1082439

Cat. No.: HY-100886 Purity: 98.02%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

BAY1082439 Chemical Structure

CAS No. : 1375469-38-7

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Description

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^[1].
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	PC3 and LNCaP cells (PTEN-null human prostate cancer cell lines)
Concentration:	0.1, 0.33, 1, 3.3, 10 μM
Incubation Time:	72 hours
Result:	Efectively inhibited cell growth by blocking the G1/S cell cycle transition and by inducing apoptosis.

In Vivo

BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Pten conditional knockout mouse model (Pb-Cre⁺;Pten^L/L, CP model)^[2]
Dosage:	75 mg/kg
Administration:	P.o.; daily for 4 weeks
Result:	Significantly decreased tumor size and P-AKT staining, nearly normal luminal architecture, and a significant reduction of Ki67-positive cells. Significantly inhibit the human prostate cancer growth.

Clinical Trial

Molecular Weight

494.54

Formula

C₂₅H₃₀N₆O₅

CAS No.

1375469-38-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CN=C1C)NC2=NC3=C(C=CC(OC[C@H](O)CN4CCOCC4)=C3OC)C5=NCCN25

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

0.1 M HCL : 16.67 mg/mL (33.71 mM; ultrasonic and warming and heat to 60°C)

DMSO : 5 mg/mL (10.11 mM; ultrasonic and adjust pH to 5 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0221 mL	10.1104 mL	20.2208 mL
5 mM	0.4044 mL	2.0221 mL	4.0442 mL
10 mM	0.2022 mL	1.0110 mL	2.0221 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 25 mg/mL (50.55 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.02%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (253 KB) RP-HPLC (246 KB)

Handling Instructions (2659 KB)

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / 0.1 M HCL	1 mM	2.0221 mL	10.1104 mL	20.2208 mL	50.5520 mL
	5 mM	0.4044 mL	2.0221 mL	4.0442 mL	10.1104 mL
	10 mM	0.2022 mL	1.0110 mL	2.0221 mL	5.0552 mL
0.1 M HCL	15 mM	0.1348 mL	0.6740 mL	1.3481 mL	3.3701 mL
	20 mM	0.1011 mL	0.5055 mL	1.0110 mL	2.5276 mL
	25 mM	0.0809 mL	0.4044 mL	0.8088 mL	2.0221 mL
	30 mM	0.0674 mL	0.3370 mL	0.6740 mL	1.6851 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAY10824391375469-38-7BAY 1082439BAY-1082439Inhibitorinhibitorinhibit

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