Bafetinib (Synonyms: INNO-406) |
Catalog No.GC35462
One-Click Copy Product Info
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Bafetinib is a dual Bcr-Abl/Lyn tyrosine kinase inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 859212-16-1
Sample solution is provided at 25 µL, 10mM.
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Bafetinib is a dual Bcr-Abl/Lyn tyrosine kinase inhibitor. Bafetinib inhibits Bcr-Abl autophosphorylation and enhances pro-apoptotic protein activity. Bafetinib can be used in research related to chronic myeloid leukemia, chronic lymphocytic leukemia, prostate cancer, and brain tumors[1-4].
In vitro, HEK-293 T cells (stably expressing human ACE2 and TMPRSS2) infected with SARS-CoV-2 Wuhan strain (MOI=0.5i.u./cell) were treated with Bafetinib (0.09, 0.9, and 9μM) for 16-18 hours. Bafetinib significantly inhibited the number of virus-infected cells and suppressed virus-induced syncytium formation[5]. ABCB1-overexpressing SW620/Ad300 and HEK/ABCB1 cells, as well as ABCG2-overexpressing NCI-H460/MX20 and HEK/ABCG2-R482 cells, were pretreated with Bafetinib (1-3 μM) for 1 hour, followed by a 2-hour [³H]-paclitaxel or [³H]-mitoxantrone accumulation assay. Bafetinib significantly increased intracellular drug accumulation and inhibited drug efflux[6].
In vivo, Balb/c mice inoculated with CT26 cells were administered Bafetinib (30mg/kg; once daily) by gavage for 10 days. Bafetinib significantly inhibited tumor growth and markedly suppressed PD-L1 expression[7]. In pain behavior experiments, C57BL/6 mice were administered Bafetinib (10mg/kg; single treatment) by gavage 30 minutes before the test. Bafetinib significantly inhibited PAR2-induced mechanical hyperalgesia[8].
References:
[1] Santos FP, Kantarjian H, Cortes J, et al. Bafetinib, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia. Curr Opin Investig Drugs. 2010 Dec;11(12):1450-65.
[2] Liu D, Jin X, Zeng Y, et al. Bafetinib enhances anti-tumor immunity by activating the NLRP3 inflammasome in macrophage. Autophagy. 2026 Apr 12:1-19.
[3] Kuroda J, Kimura S, Strasser A, 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.
[4] Milara J, Martinez-Losa M, Sanz C, et al. Bafetinib inhibits functional responses of human eosinophils in vitro. Eur J Pharmacol. 2013 Sep 5;715(1-3):172-80.
[5] Serra A, Fratello M, Federico A, et al. Computationally prioritized drugs inhibit SARS-CoV-2 infection and syncytia formation. Brief Bioinform. 2022 Jan 17;23(1):bbab507.
[6] Zhang YK, Zhang GN, Wang YJ, et al. Bafetinib (INNO-406) reverses multidrug resistance by inhibiting the efflux function of ABCB1 and ABCG2 transporters. Sci Rep. 2016 May 9;6:25694.
[7] Chen X, Du Q, Guo H, et al. Bafetinib Suppresses the Transcription of PD-L1 Through c-Myc in Lung Cancer. Front Pharmacol. 2022 Jun 2;13:897747.
[8] Grace MS, Lieu T, Darby B, 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.
| Cell experiment [1]: | |
Cell lines | HEK-293 T cells stably expressing human ACE2 and TMPRSS2 (HEK-293 T-AT) |
Preparation Method | HEK-293 T-AT cells were treated with Bafetinib at different concentrations and infected with SARS-CoV-2 (Wuhan strain) at a multiplicity of infection (MOI) of 0.5 infectious units per cell for 16-18 hours. |
Reaction Conditions | 0.09, 0.9, and 9μM; 16-18h |
Applications | Bafetinib showed a statistically significant inhibition of the number of virus-infected cells (relative infection value of 0.69). Bafetinib also strongly inhibits viral-induced syncytia formation. |
| Animal experiment [2]: | |
Animal models | Male Balb/c mice (6 weeks) and Male immunodeficient nude mice |
Preparation Method | 5 x 10⁶ murine colorectal adenocarcinoma CT26 cells were subcutaneously inoculated into mice. The mice were randomly divided into two groups and treated with 5% CMC-Na or Bafetinib (30mg/kg daily) dispersed in 5% CMC-Na intragastrically for 10 days. |
Dosage form | 30mg/kg; intragastric administration; daily for 10 days |
Applications | Bafetinib treatment significantly inhibited tumor growth compared with the control group. Bafetinib significantly inhibited the expression of PD-L1 in mouse tumors. In immunodeficient nude mouse models, Bafetinib didn't inhibit tumor growth, although lower PD-L1 expression was observed. |
References: | |
| Cas No. | 859212-16-1 | SDF | |
| Synonyms | INNO-406 | ||
| Chemical Name | (S)-N-(3-([4,5'-bipyrimidin]-2-ylamino)-4-methylphenyl)-4-((3-(dimethylamino)pyrrolidin-1-yl)methyl)-3-(trifluoromethyl)benzamide | ||
| Canonical SMILES | O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CN=CN=C3)=N2)=C1)C4=CC=C(CN5C[C@@H](N(C)C)CC5)C(C(F)(F)F)=C4 | ||
| Formula | C30H31F3N8O | M.Wt | 576.62 |
| Solubility | DMSO: ≥ 42 mg/mL (72.84 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7342 mL | 8.6712 mL | 17.3424 mL |
| 5 mM | 346.8 μL | 1.7342 mL | 3.4685 mL |
| 10 mM | 173.4 μL | 867.1 μL | 1.7342 mL |
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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 saline, 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.
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)