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Nilotinib hydrochloride monohydrate Bcr-Abl inhibitor

Name: Nilotinib hydrochloride monohydrate
Brand: Selleck Chemicals
SKU: S4895
Availability: InStock
Rating: 5 (12 reviews)

Cat.No.S4895

Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.

Chemical Structure

Molecular Weight: 583.99

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S489501 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.98%

99.98

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Chemical Information, Storage & Stability

Molecular Weight	583.99	Formula	C₂₈H₂₅ClF₃N₇O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	923288-90-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Tasigna, AMN-107 hydrochloride monohydrate			Smiles	O.Cl.CC1=C[N](C=N1)C2=CC(=CC(=C2)NC(=O)C3=CC(=C(C)C=C3)NC4=NC=CC(=N4)C5=CN=CC=C5)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (171.23 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.65mg/ml (2.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.425mg/ml (0.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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	AMPK ^[1] Bcr-Abl ^[1] (in Murine myeloid progenitor cells) 30 nM
References	[1] https://pubmed.ncbi.nlm.nih.gov/17068153/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06409936	Not yet recruiting	CML Chronic Phase\|Chronic Myeloid Leukemia Chronic Phase\|Chronic Myeloid Leukemia BCR/ABL-Positive\|Chronic Myeloid Leukemia	Gruppo Italiano Malattie EMatologiche dell''Adulto\|Fundacion Espanola para la Curacion de la Leucemia Mieloide Cronica	September 2024	Phase 2
NCT05185947	Recruiting	Gynecologic Cancer\|Gynecologic Neoplasms\|Peritoneal Carcinomatosis\|Peritoneal Neoplasms\|Ovarian Cancer\|Ovarian Neoplasms\|Colorectal Cancer\|Colorectal Neoplasms\|Appendiceal Cancer\|Appendiceal Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	October 13 2022	Phase 2
NCT04326933	Unknown status	Patients Diagnosed as Chronic Meyloid Leukemia	Assiut University	January 1 2020	--
NCT04002674	Recruiting	Dementia With Lewy Bodies	Georgetown University\|National Institutes of Health (NIH)	July 1 2019	Phase 2

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Handling Instructions

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