ON 146040

CAS# 1404231-34-0

ON 146040

Catalog No. BCC8058----Order now to get a substantial discount!

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ON 146040: 5mg $460 In Stock
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Chemical structure

ON 146040

3D structure

Chemical Properties of ON 146040

Cas No. 1404231-34-0 SDF Download SDF
PubChem ID 73297262 Appearance Powder
Formula C24H23N7O3S M.Wt 489.55
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
Chemical Name (7Z)-2-[4-(4-methylpiperazin-1-yl)anilino]-7-[(4-nitrophenyl)methylidene]-5H-pyrimido[4,5-b][1,4]thiazin-6-one
SMILES CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C4C(=N3)SC(=CC5=CC=C(C=C5)[N+](=O)[O-])C(=O)N4
Standard InChIKey PKCHFYZACODWAI-STZFKDTASA-N
Standard InChI InChI=1S/C24H23N7O3S/c1-29-10-12-30(13-11-29)18-8-4-17(5-9-18)26-24-25-15-20-23(28-24)35-21(22(32)27-20)14-16-2-6-19(7-3-16)31(33)34/h2-9,14-15H,10-13H2,1H3,(H,27,32)(H,25,26,28)/b21-14-
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ON 146040

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

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

ON 146040 Dilution Calculator

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ON 146040 Molarity Calculator

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Preparing Stock Solutions of ON 146040

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0427 mL 10.2135 mL 20.4269 mL 40.8538 mL 51.0673 mL
5 mM 0.4085 mL 2.0427 mL 4.0854 mL 8.1708 mL 10.2135 mL
10 mM 0.2043 mL 1.0213 mL 2.0427 mL 4.0854 mL 5.1067 mL
50 mM 0.0409 mL 0.2043 mL 0.4085 mL 0.8171 mL 1.0213 mL
100 mM 0.0204 mL 0.1021 mL 0.2043 mL 0.4085 mL 0.5107 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on ON 146040

ON 146040 is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways; inhibits PI3K α/δ isoforms with IC50 of 14/20 nM.

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Description

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

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