ON 146040

Cat. No.: HY-12338 Purity: 95.05%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

ON 146040 is a potent PI3Kα and PI3Kδ (IC₅₀≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC₅₀<150 nM).

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

ON 146040 Chemical Structure

CAS No. : 1404231-34-0

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 323	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 323	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

ON 146040 is a potent PI3Kα and PI3Kδ (IC₅₀≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC₅₀<150 nM).

IC₅₀ & Target^[1]

PI3Kα

14 nM (IC₅₀)

PI3Kδ

20 nM (IC₅₀)

PI3Kγ

1 μM (IC₅₀)

PI3Kβ

3 μM (IC₅₀)

In Vitro

In biochemical testing, ON 146040 inhibits PI3Kα/ PI3Kδ isoforms (IC₅₀≈14 and 20 nM, respectively) without having a major effect on PI3Kβ/ PI3Kγ isoforms (IC₅₀≈3 and 1 μM, respectively). ON 146040 is also found to inhibit Abl1 and several mutant versions of this kinase (IC₅₀<150 nM), although ON 146040 is not found to be active against the T315I mutant. ON 146040 represents the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways. ON 146040 disrupts the oncogenic activity of both STAT3 and STAT5 by targeting upstream activators, including PI3K α and δ isoforms as well as wild type and mutant BCR-ABL. ON 146040 is highly potent in killing hematologic tumor cells with IC₅₀ values in the 150 to 1,000 nM range. Following treatment with ON 146040, STAT3 and STAT5 phosphorylation are down-regulated in leukemia and myeloma cells^[1].

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

Molecular Weight

489.55

Formula

C₂₄H₂₃N₇O₃S

CAS No.

1404231-34-0

Appearance

Solid

Color

Brown to reddish brown

SMILES

CN(CC1)CCN1C(C=C2)=CC=C2NC3=NC(S/C(C(N4)=O)=C\C5=CC=C([N+]([O-])=O)C=C5)=C4C=N3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (51.07 mM; ultrasonic and warming and heat to 60°C; 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	2.0427 mL	10.2135 mL	20.4269 mL
5 mM	0.4085 mL	2.0427 mL	4.0854 mL
10 mM	0.2043 mL	1.0213 mL	2.0427 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 (protect from light). 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 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: 95.05%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (249 KB) HNMR (267 KB) RP-HPLC (255 KB) MS (183 KB)

Handling Instructions (2659 KB)

References

[1]. Targeting oncogenic STAT3 and STAT5 signaling with on 146040, a small molecule inhibitor of PI3K α/δ and BCR-ABL.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.0427 mL	10.2135 mL	20.4269 mL	51.0673 mL
	5 mM	0.4085 mL	2.0427 mL	4.0854 mL	10.2135 mL
	10 mM	0.2043 mL	1.0213 mL	2.0427 mL	5.1067 mL
	15 mM	0.1362 mL	0.6809 mL	1.3618 mL	3.4045 mL
	20 mM	0.1021 mL	0.5107 mL	1.0213 mL	2.5534 mL
	25 mM	0.0817 mL	0.4085 mL	0.8171 mL	2.0427 mL
	30 mM	0.0681 mL	0.3404 mL	0.6809 mL	1.7022 mL
	40 mM	0.0511 mL	0.2553 mL	0.5107 mL	1.2767 mL
	50 mM	0.0409 mL	0.2043 mL	0.4085 mL	1.0213 mL

ON 146040 Related Classifications

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:

ON 1460401404231-34-0ON146040ON-146040PI3KBcr-AblPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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