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ONO-4059 analogue BTK inhibitor

Name: ONO-4059 analogue
Brand: Selleck Chemicals
SKU: S7877
Rating: 5 (1 reviews)

Cat.No.S7877

ONO-4059 analogue (ONO-WG-307) is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with an IC50 of 23.9 nM. Phase 1.

Chemical Structure

Molecular Weight: 456.50

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Quality Control

Batch: Purity: 99.82%

99.82

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2
Other BTK Inhibitors	Catadegbrutinib (BGB-16673) Spebrutinib (AVL-292) tirabrutinib(ONO-4059) hydrochloride CGI1746 LFM-A13 CNX-774 Evobrutinib BMS-935177 Fenebrutinib (GDC-0853) Branebrutinib (BMS-986195)

Chemical Information, Storage & Stability

Molecular Weight	456.50	Formula	C₂₅H₂₄N₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1351635-67-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ONO-WG-307			Smiles	C=CC(=O)N1CCCC(C1)N2C3=NC=NC(=C3N(C2=O)C4=CC=C(C=C4)OC5=CC=CC=C5)N

Solubility

In vitro
Batch:

DMSO : 30 mg/mL (65.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	BTK 23.9 nM
In vitro	In TMD-8 cells, ONO-4059 inhibits cell growth with an IC50 of 3.59 nM, and induces cell apoptosis. The combination of ONO-4059 with doxorubicin, etoposide, vincristine or dexamethasone causes an increased apoptosis ratio.
References	[1] http://www.bloodjournal.org/content/122/21/5151

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