KX2 391
KX2-391
CAS: 897016-82-9
Molecular Formula: C26H29N3O3
KX2 391 - Names and Identifiers
KX2 391 - Physico-chemical Properties
| Molecular Formula | C26H29N3O3 |
| Molar Mass | 431.53 |
| Density | 1.169 |
| Boling Point | 680.9±55.0 °C(Predicted) |
| pKa | 14.73±0.46(Predicted) |
| Storage Condition | -20℃ |
| Use | Tirbanibulin (KX2-391) is a peptide-like Src inhibitor that targets the polypeptide substrate binding site of Src and has a GI50 of 9-60 nM for a variety of cancer cell strains. |
| In vitro study | KX2-391 is a Src inhibitor that acts directly on the Src substrate pocket. KX2-391 vs Huh7 (GI 50=9 nM),PLC/PRF/5 (GI 50=13 nM),Hep3B (GI 50=26 nM), and HepG2 (GI 50=60 nM), four hepatocellular carcinoma (HCC) cell lines showed steep dose response curves. KX2-391 is able to inhibit certain leukemic cells that are resistant to commercially available drugs, such as cell lines derived from chronic leukemic cells loaded with the T3151 mutant. KX2-391 was evaluated in a designed Src-driven cell growth assay with GI50 of 23 nM and 39 nM in NIH3T3/c-Src527F and SYF/c-Src527F cells, respectively. |
| In vivo study | In preclinical animal models of cancer, oral administration of KX2-391 inhibits the growth of primary tumors and inhibits metastasis. |
KX2 391 - Reference
| Reference Show more | 1: Li X, Liu X, Deng R, Gao S, Yu H, Huang K, Jiang Q, Liu R, Li X, Zhang L, Zhou H, Yang C. Nintedanib Inhibits Wnt3a-Induced Myofibroblast Activation by Suppressing the Src/β-Catenin Pathway. Front Pharmacol. 2020 Mar 16;11:310. doi: 10.3389/fphar.2020.00310. PMID: 32231574; PMCID: PMC7087487. 2: Niu L, Yang J, Yan W, Yu Y, Zheng Y, Ye H, Chen Q, Chen L. Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of β-tubulin explains KXO1's low clinical toxicity. J Biol Chem. 2019 Nov 29;294(48):18099-18108. doi: 10.1074/jbc.RA119.010732. Epub 2019 Oct 18. PMID: 31628188; PMCID: PMC6885616. 3: Wei J, Ma L, Li C, Pierson CR, Finlay JL, Lin J. Targeting Upstream Kinases of STAT3 in Human Medulloblastoma Cells. Curr Cancer Drug Targets. 2019;19(7):571-582. doi: 10.2174/1568009618666181016165604. PMID: 30332965; PMCID: PMC6533162. 4: Smolinski MP, Bu Y, Clements J, Gelman IH, Hegab T, Cutler DL, Fang JWS, Fetterly G, Kwan R, Barnett A, Lau JYN, Hangauer DG. Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). J Med Chem. 2018 Jun 14;61(11):4704-4719. doi: 10.1021/acs.jmedchem.8b00164. Epub 2018 Apr 17. PMID: 29617135. |
KX2 391 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.317 ml | 11.587 ml | 23.173 ml |
| 5 mM | 0.463 ml | 2.317 ml | 4.635 ml |
| 10 mM | 0.232 ml | 1.159 ml | 2.317 ml |
| 5 mM | 0.046 ml | 0.232 ml | 0.463 ml |
Last Update：2024-01-02 23:10:35
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Product Name: Tirbanibulin Visit Supplier Webpage Request for quotationCAS: 897016-82-9
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: KX2-391 Visit Supplier Webpage Request for quotationCAS: 897016-82-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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