Tirbanibulin dihydrochloride
Based on 9 publication(s) in Google Scholar
Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
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- 純度: 98.02%
- CAS 番号: 1038395-65-1
- 分子式: C26H31Cl2N3O3
- 分子量:504.45
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Tirbanibulin dihydrochloride
More- Cancer Cell. 2024 Apr 8;42(4):682-700.e12. [Abstract]
- Nat Commun. 2024 Sep 9;15(1):7885. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Exp Clin Cancer Res. 2025 Jul 8;44(1):195. [Abstract]
- Microbiol Spectr. 2026 Mar 17:e0362025. [Abstract]
- J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]
- Brain Res. 2020 Jun 1:1736:146782. [Abstract]
- University of Colorado Denver. 2024.
- bioRxiv. 2023 Dec 14.
Customer Validation & Images
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Cell Migration/Invasion Assay
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Flow Cytometry
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Cell Imaging/Staining
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WB
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Cell Proliferation/Viability Assay
生物活性
GI50: 9 nM (Src HuH7), 13 nM (Src PLC/PRF/5), 26 nM (Src Hep3B), 60 nM (Src HepG2)
Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI50=9 nM), PLC/PRF/5 (GI50=13 nM), Hep3B (GI50=26 nM), and HepG2 (GI50=60 nM), four hepatic cell cancer (HCC) cell lines[1]. Tirbanibulin (KX2-391) is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. Tirbanibulin (KX2-391) is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1038395-65-1
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性状 Solid
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分子量 504.45
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分子式 C26H31Cl2N3O3
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Color Light yellow to yellow
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SMILES
O=C(CC1=NC=C(C2=CC=C(OCCN3CCOCC3)C=C2)C=C1)NCC4=CC=CC=C4.Cl.Cl
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別名
KX2-391 dihydrochloride; KX-01 dihydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (9)
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Journal Impact Factor
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Most Recent
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Cancer Cell
PDGFRα+ITGA11+ fibroblasts foster early-stage cancer lymphovascular invasion and lymphatic metastasis via ITGA11-SELE interplay. [Abstract]2024 Apr 8;42(4):682-700.e12. PMID: 38428409 -
Nat Commun
Defective N-glycosylation of IL6 induces metastasis and tyrosine kinase inhibitor resistance in lung cancer. [Abstract]2024 Sep 9;15(1):7885. PMID: 39251588
Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 9;15(1):7885. [Abstract]
Effect of IL6 antibody (5 μg/mL), JAK-STAT3 inhibitors (S3I-201 = 10 μM, ruxolitinib = 2.5 μM), and SRC inhibitors (PP1 = 10 μM, PP2 = 10 μM, Tirbanibulin = 10 μM) on the migration of AS2-IL6-WT and AS2-IL6-N73Q cells through the space made by culture inserts. Images were obtained at 0 and 24 h.
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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 -
J Exp Clin Cancer Res
Genomic profiling of a collection of patient-derived xenografts and cell lines identified ixabepilone as an active drug against chemo-resistant osteosarcoma. [Abstract]2025 Jul 8;44(1):195. PMID: 40624718 -
Microbiol Spectr
Repurposing flufenamic acid as a putative PmrB-directed adjuvant to restore colistin activity in Klebsiella pneumoniae. [Abstract]2026 Mar 17:e0362025. PMID: 41842337 -
J Biol Chem
Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of β-tubulin explains KXO1's low clinical toxicity. [Abstract]2019 Nov 29;294(48):18099-18108. PMID: 31628188
Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]
Tirbanibulin (KXO1; 0, 12.5, 25, 50, 100 nM; 16 h) induced cell cycle arrest at G2/M phase in HeLa, HepG2, and H460 cells.
Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]
HeLa cells were treated with 100 nM paclitaxel (PTX), 100 nM vinblastine (Vin), 100 nM colchicine (Col), or 30 or 100 nM Tirbanibulin(KXO1) for 16 h, and microtubule morphology was monitored by immunofluorescence.
Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]
Tirbanibulin (KXO1; 1 5 25 nM; 16 h) was incubated for 2 h before being treated with 100 μM EBI for another 2 h. Tirbanibulin inhibited the formation of the EBI-tubulin complex, but vinblastine did not, thus confirming KXO1 binding to the colchicine site on tubulin.
Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]
Tirbanibulin (KXO1; 0-10000 nM; 5 days) reduced cell viability at 100000 nM in HeLa cells.
Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]
Tirbanibulin (KXO1; 0-10000 nM; 10 h) was a totally reversible tubulin inhibitor.
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Brain Res
Donepezil promotes neurogenesis via Src signaling pathway in a rat model of chronic cerebral hypoperfusion. [Abstract]2020 Jun 1:1736:146782. PMID: 32184165 -
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溶剤 & 溶解度
H2O : 100 mg/mL (198.24 mM; Need ultrasonic)
DMSO : 33.33 mg/mL (66.07 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (4.96 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.96 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
プロトコル
Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 are routinely cultured and maintained in basal medium containing 2% fetal bovine serum (FBS) at 37°C and 5% CO2. Cells are seeded at 4.0×103/190 μL and 8.0×103/190 μL per well of 96-well plate in basal medium containing 1.5% FBS. These are cultured overnight at 37°C and 5% CO2 prior to the addition of Tirbanibulin (KX2-391), at concentrations ranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten μLs of 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/mL) is then added to each well on day 3 and cells incubated for 4 hours. The formazan product is dissolved with 10% SDS in dilute HCl. Optical density at 570 nm is measured. For comparison of activity and potency, parallel experiments are performed using Tirbanibulin (KX2-391). Growth inhibition curves, 50% inhibition concentration (GI50), and 80% inhibition concentration (GI80) are determined using GraphPad Prism 5 statistical software. Data are normalized to represent percentage of maximum response as well as reported in optical density at wavelength of 570 nm (OD570) signal format.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (274 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Lau GM, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig Dis Sci, 2009, 54(7), 1465-1474. [Content Brief]
[2]. Fallah-Tafti A, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur J Med Chem, 2011, 46(10), 4853-4858. [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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.9824 mL | 9.9118 mL | 19.8236 mL | 49.5589 mL |
| 5 mM | 0.3965 mL | 1.9824 mL | 3.9647 mL | 9.9118 mL | |
| 10 mM | 0.1982 mL | 0.9912 mL | 1.9824 mL | 4.9559 mL | |
| 15 mM | 0.1322 mL | 0.6608 mL | 1.3216 mL | 3.3039 mL | |
| 20 mM | 0.0991 mL | 0.4956 mL | 0.9912 mL | 2.4779 mL | |
| 25 mM | 0.0793 mL | 0.3965 mL | 0.7929 mL | 1.9824 mL | |
| 30 mM | 0.0661 mL | 0.3304 mL | 0.6608 mL | 1.6520 mL | |
| 40 mM | 0.0496 mL | 0.2478 mL | 0.4956 mL | 1.2390 mL | |
| 50 mM | 0.0396 mL | 0.1982 mL | 0.3965 mL | 0.9912 mL | |
| 60 mM | 0.0330 mL | 0.1652 mL | 0.3304 mL | 0.8260 mL | |
| H2O | 80 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6195 mL |
| 100 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4956 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Tirbanibulin dihydrochloride 関連分類
HY-10340A 関連分類
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