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Tirbanibulin

Catalog No. T6345 CAS 897016-82-9

Synonyms: KX2-391, KX-01

Tirbanibulin (KX2-391) is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-Clinicalal animal models of colon, pancreatic, prostate and breast cancer. It is a substrate-targeted kinase inhibitor. KX2-391, belongs to an emerging new family of targeted cancer treatments called protein kinase inhibitors.

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Tirbanibulin, CAS 897016-82-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 35.00
5 mg	In stock	$ 57.00
10 mg	In stock	$ 70.00
25 mg	In stock	$ 143.00
50 mg	In stock	$ 279.00
100 mg	In stock	$ 483.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 99.67%

Purity: 99.43%

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Description	Tirbanibulin (KX2-391) is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-Clinicalal animal models of colon, pancreatic, prostate and breast cancer. It is a substrate-targeted kinase inhibitor. KX2-391, belongs to an emerging new family of targeted cancer treatments called protein kinase inhibitors.
Targets&IC50	Src (HuH-7):9 nM(GI50), Src (HepG2):60 nM(GI50), Src (Hep3B):26 nM(GI50), Src (PLC/PRF/5):13 nM(GI50)
In vitro	KX2-391 is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI 50 = 9 nM), PLC/PRF/5 (GI 50 = 13 nM), Hep3B (GI 50 = 26 nM), and HepG2 (GI 50 = 60 nM), four hepatic cell cancer (HCC) cell lines. [1] 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. 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]
In vivo	In pre-Clinicalal animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis. [2]
Cell Research	Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 (NutriCyte, Buffalo, NY) 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 KX2-391, at concentrations ranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten microliters 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 by using BioTek Synergy HT multiplatform microplate reader. For comparison of activity and potency, parallel experiments are performed using 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.</ (Only for Reference)

Synonyms	KX2-391, KX-01
Molecular Weight	431.53
Formula	C26H29N3O3
CAS No.	897016-82-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (185.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Lau GM, et al, Dig Dis Sci, 2009, 54(7), 1465-1474. 2. Fallah-Tafti A, et al, Eur J Med Chem, 2011, 46(10), 4853-4858. 3. Zhang X, Xu H, Bi X, et al. Src acts as the target of matrine to inhibit the proliferation of cancer cells by regulating phosphorylation signaling pathways[J]. 2020

Citations

1. Chen J, Lei C, Nie D, et al.Inorganic arsenic exposure promotes malignant progression by HDAC6‐mediated down‐regulation of HTRA1.Journal of Applied Toxicology.2023

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library EMA Approved Drug Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Approved Drug Library Microtubule-Targeted Compound Library Kinase Inhibitor Library

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Keywords

Tirbanibulin 897016-82-9 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Src Microtubule Associated Microtubule/Tubulin Inhibitor inhibit KX 01 KX2-391 KX-01 KX01 inhibitor

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