Bafetinib
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.02%
- CAS 番号: 859212-16-1
- 分子式: C30H31F3N8O
- 分子量:576.62
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Anti-Infection Compound Library
HY-L002
-
Apoptosis Compound Library
HY-L003
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
-
Reprogramming Compound Library
HY-L039
-
Anti-COVID-19 Compound Library
HY-L052
-
Cytoskeleton Compound Library
HY-L060
-
Orally Active Compound Library
HY-L061
-
Chemical Probe Library
HY-L063
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Blood Cancer Compound Library
HY-L079
-
Anti-Parkinson's Disease Compound Library
HY-L085
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Angiogenesis-Related Compound Library
HY-L088
-
Human Metabolite Library
HY-L123
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Heterocyclic Compound Library
HY-L138
-
Pain-Related Compound Library
HY-L139
-
Membrane Protein-targeted Compound Library
HY-L149
-
Cell Death Library
HY-L162
-
Anti-Hematopathy Compound Library
HY-L171
-
Multi-Target Compound Library
HY-L176
-
Mitophagy Compound Library
HY-L180
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Posttranslational Modification Library
HY-L226
MedChemExpress（MCE）の使用を引用している文献 Bafetinib
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Mil Med Res. 2023 Jun 5;10(1):25. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Redox Biol. 2023 Nov:67:102898. [Abstract]
- Br J Haematol. 2025 Apr 20. [Abstract]
- Food Chem Toxicol. 2020 Jan;135:110924. [Abstract]
- J Cancer. 2019 Jan 29;10(5):1197-1208. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Behav Brain Res. 2026 Jun 5:507:116187. [Abstract]
- Hong Kong Polytechnic University. 2025.
- Immunologie. 2023 Feb 14.
- SSRN. 2022 Nov 21.
- Technical University of Munich. 24.01.2018.
Customer Validation & Images
-
WB
生物活性
|
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] |
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.
-
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 859212-16-1
-
性状 Solid
-
分子量 576.62
-
分子式 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
-
別名
INNO-406; NS-187
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (14)
-
Journal Impact Factor
-
Most Recent
-
Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Mil Med Res
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
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 -
-
-
-
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
-
データシート (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)
-
取扱説明書 (2659 KB)
参考文献
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
Powered by Bioz