Cat. No.: HY-50868

Bafetinib

(Synonyms: INNO-406; NS-187)

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph⁺ leukemia cells. Bafetinib has antitumor activity.

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Pureté: 99.02%
CAS No.: 859212-16-1
Formule: C₃₀H₃₁F₃N₈O
Masse moléculaire:576.62

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Bafetinib Chemical Structure

CAS No.: 859212-16-1

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

Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (14)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform Bcr-Abl :

Abl
Bcr-Abl

Voir tous les produits spécifiques à Isoform Src :

Cellular Effect

Cell Line	Type	Value	Description	References
K562	IC₅₀	11 nM Compound: 9b	Antiproliferative activity against K562 cells Antiproliferative activity against K562 cells	[PMID: 16332440]
Sf9	IC₅₀	11 nM Compound: 8, INNO-406, NS-187	Inhibition of human Lyn kinase expressed in Sf9 cells Inhibition of human Lyn kinase expressed in Sf9 cells	[PMID: 17376680]
Sf9	IC₅₀	26 nM Compound: 8, INNO-406, NS-187	Inhibition of human Abl kinase expressed in Sf9 cells Inhibition of human Abl kinase expressed in Sf9 cells	[PMID: 17376680]
U-937	IC₅₀	10 μM Compound: 9b	Antiproliferative activity against U937 cells Antiproliferative activity against U937 cells	[PMID: 16332440]

In Vitro

Bafetinib (0.625, 1.25, 2.5 μM,24 h) inhibits the transcription of PD-L1 in lung cancer cell H292 by c-Myc^[1].

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

Western Blot Analysis^[1]

Cell Line:

H292
Concentration:

0.625, 1.25, 2.5 μM
Incubation Time:

24 h
Result:

Inhibited the expression of PD-L1 and c-Myc.

In Vivo

Bafetinib (30 mg/kg/day, orally, for 10 consecutive days) inhibits the expression of PD-L1 in mouse lung cancer^[1].
Bafetinib (10 mg/kg, gavage, single dose) alleviates pain in mice by inhibiting PAR2-induced TRPV4 channel activation^[2].

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

Animal Model:

Murine inflammatory pain model^[2]
Dosage:

10 mg/kg
Administration:

i.g.
Result:

Inhibited PAR2-induced mechanical hyperalgesia.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 859212-16-1
Appearance Solid
Masse moléculaire 576.62
Formule C₃₀H₃₁F₃N₈O
Color Light yellow to yellow
SMILES

O=C(C1=CC=C(C(C(F)(F)F)=C1)CN2C[C@@H](N(C)C)CC2)NC3=CC=C(C)C(NC4=NC=CC(C5=CN=CN=C5)=N4)=C3
Synonyms

INNO-406; NS-187
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All WB

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Mil Med Res

Aspartoacylase suppresses prostate cancer progression by blocking LYN activation. [Abstract]

2023 Jun 5;10(1):25. PMID: 37271807
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Redox Biol

TNFα counteracts interleukin-10 anti-inflammatory pathway through the NOX2-Lyn-SHP-1 axis in human monocytes. [Abstract]

2023 Nov:67:102898. PMID: 37757542
Br J Haematol

Development and characterization of the novel MYD88 mutated, 6q deleted BCWM.2 cell line for Waldenström macroglobulinaemia. [Abstract]

2025 Apr 20. PMID: 40254718
Food Chem Toxicol

Quercetin as a Lyn kinase inhibitor inhibits IgE-mediated allergic conjunctivitis. [Abstract]

2020 Jan;135:110924. PMID: 31672514
J Cancer

Lyn Kinase Promotes the Proliferation of Malignant Melanoma Cells through Inhibition of Apoptosis and Autophagy via the PI3K/Akt Signaling Pathway. [Abstract]

2019 Jan 29;10(5):1197-1208. PMID: 30854129

Bafetinib purchased from MedChemExpress. Usage Cited in: J Cancer. 2019 Jan 29;10(5):1197-1208. [Abstract]

Western blot shows the effects of Bafetinib on expression of Akt, p-Akt, Cyclin D1, cleaved-Caspase3, Caspase9, Bcl-2, LC3II/I, P62 and Lyn.
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
Behav Brain Res

Integrative multi-omics identifies lyn-mediated microglial activation as a key driver of central post-stroke pain. [Abstract]

2026 Jun 5:507:116187. PMID: 41912093
Hong Kong Polytechnic University

2025.
Immunologie

2023 Feb 14.
SSRN

2022 Nov 21.
Technical University of Munich

24.01.2018.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (173.42 mM; Need ultrasonic; 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

1.7342 mL

8.6712 mL

17.3424 mL

5 mM

0.3468 mL

1.7342 mL

3.4685 mL

10 mM

0.1734 mL

0.8671 mL

1.7342 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 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)
Instruction de manipulation (2659 KB)

Références

[1]. Chen X, et al. Bafetinib Suppresses the Transcription of PD-L1 Through c-Myc in Lung Cancer. Front Pharmacol. 2022 Jun 2;13:897747. [Content Brief]

[2]. Grace MS, et al. The tyrosine kinase inhibitor bafetinib inhibits PAR2-induced activation of TRPV4 channels in vitro and pain in vivo. Br J Pharmacol. 2014 Aug;171(16):3881-94. [Content Brief]

[3]. Kuroda J, et al. Apoptosis-based dual molecular targeting by INNO-406, a second-generation Bcr-Abl inhibitor, and ABT-737, an inhibitor of antiapoptotic Bcl-2 proteins, against Bcr-Abl-positive leukemia. Cell Death Differ. 2007 Sep;14(9):1667-77. [Content Brief]

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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7342 mL	8.6712 mL	17.3424 mL	43.3561 mL
	5 mM	0.3468 mL	1.7342 mL	3.4685 mL	8.6712 mL
	10 mM	0.1734 mL	0.8671 mL	1.7342 mL	4.3356 mL
	15 mM	0.1156 mL	0.5781 mL	1.1562 mL	2.8904 mL
	20 mM	0.0867 mL	0.4336 mL	0.8671 mL	2.1678 mL
	25 mM	0.0694 mL	0.3468 mL	0.6937 mL	1.7342 mL
	30 mM	0.0578 mL	0.2890 mL	0.5781 mL	1.4452 mL
	40 mM	0.0434 mL	0.2168 mL	0.4336 mL	1.0839 mL
	50 mM	0.0347 mL	0.1734 mL	0.3468 mL	0.8671 mL
	60 mM	0.0289 mL	0.1445 mL	0.2890 mL	0.7226 mL
	80 mM	0.0217 mL	0.1084 mL	0.2168 mL	0.5420 mL
	100 mM	0.0173 mL	0.0867 mL	0.1734 mL	0.4336 mL

Bafetinib

14 Cited Publications

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Bafetinib

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Heterocyclic Compound Library

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Publications Citing Use of MedChemExpress (MCE) Bafetinib

Voir tous les produits spécifiques à Isoform Bcr-Abl

Voir tous les produits spécifiques à Isoform Src

Activité biologique

Chemical Information

Publications (14)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Bafetinib Related Classifications

Cat. No.: HY-50868