Cat. No.: HY-12338

ON 146040

Customer Review

Based on 1 Customer Validation

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.

Purity: 95.05%
CAS No.: 1404231-34-0
Formula: C₂₄H₂₃N₇O₃S
Molecular Weight:489.55

Storage:

4°C, protect from light

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

ON 146040 Chemical Structure

CAS No.: 1404231-34-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

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)

All PI3K Isoforms :

All Bcr-Abl Isoforms :

Abl
Bcr-Abl

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.

Chemical Information

CAS No. 1404231-34-0
Appearance Solid
Molecular Weight 489.55
Formula C₂₄H₂₃N₇O₃S
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

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ON 146040

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All PI3K Isoforms

All Bcr-Abl Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ON 146040 Related Classifications

Cat. No.: HY-12338