Tirbanibulin Mesylate (KX2-391 (Mesylate)) (Synonyms: KX2-391 Mesylate; KX01 Mesylate) |
| カタログ番号GC34109 |
メシル酸チルバニブリン (KX2-391 (メシル酸)) (KX2-391 メシル酸) は、Src のペプチド基質部位を標的とする Src の阻害剤であり、癌細胞株で GI50 は 9 ～ 60 nM です。
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Cas No.: 1080645-95-9
Sample solution is provided at 25 µL, 10mM.
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Tirbanibulin (Mesylate) (KX2-391 (Mesylate)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. Tirbanibulin (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].
Orally administered Tirbanibulin (KX2-391) is shown to inhibit primary tumor growth and to suppress metastasis, in pre-clinical animal models of cancer[2].
[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. [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.
Cell experiment: | 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. |
References: [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. | |
| Cas No. | 1080645-95-9 | SDF | |
| 同義語 | KX2-391 Mesylate; KX01 Mesylate | ||
| Canonical SMILES | O=C(NCC1=CC=CC=C1)CC2=NC=C(C3=CC=C(OCCN4CCOCC4)C=C3)C=C2.CS(=O)(O)=O | ||
| Formula | C27H33N3O6S | M.Wt | 527.63 |
| 溶解度 | DMSO : ≥ 57 mg/mL (108.03 mM) | Storage | Store at -20°C, protect from light, stored under nitrogen |
| 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 | 1.8953 mL | 9.4763 mL | 18.9527 mL |
| 5 mM | 379.1 μL | 1.8953 mL | 3.7905 mL |
| 10 mM | 189.5 μL | 947.6 μL | 1.8953 mL |
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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