Tirbanibulin

製品コードS2700 バッチS270002

化学情報

	Synonyms	KX 01	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₆H₂₉N₃O₃
	分子量	431.53	CAS No.	897016-82-9
Solubility (25°C)*	体外	DMSO	86 mg/mL (199.29 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Tirbanibulin, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.
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-clinical animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis. ^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Huh7, PLC/PRF/5, Hep3B, and HepG2 cell lines
	濃度	6,564 to 0.012 nM
	反応時間	3 days
	実験の流れ	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.

参考

カスタマーフィードバック

: , , Neurotox Res, 2015, 27(4):384-98.

: Data from [Data independently produced by , , Front Immunol, 2018, 9:2433]

: Data from [Data independently produced by , , Oncotarget, 2016, 7(31):50027-50042]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Tumor Cell-Intrinsic CD96 Mediates Chemoresistance and Cancer Stemness by Regulating Mitochondrial Fatty Acid β-Oxidation [ Adv Sci (Weinh), 2023, 10(7):e2202956]	PubMed: 36581470
THY1 (CD90) Maintains the Adherens Junctions in Nasopharyngeal Carcinoma via Inhibition of SRC Activation [ Cancers (Basel), 2023, 15(7)2189]	PubMed: 37046850
Intracellular CYTL1, a novel tumor suppressor, stabilizes NDUFV1 to inhibit metabolic reprogramming in breast cancer [ Signal Transduct Target Ther, 2022, 7(1):35]	PubMed: 35115484
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7]	PubMed: 35332332
Procr functions as a signaling receptor and is essential for the maintenance and self-renewal of mammary stem cells [ Cell Rep, 2022, 38(12):110548]	PubMed: 35320720
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening [ Cancers (Basel), 2022, 14(6)1575]	PubMed: 35326726
Exendin-4, a glucagon-like peptide receptor agonist, facilitates osteoblast differentiation via connexin43 [ Endocrine, 2021, 10.1007/s12020-021-02664-7]	PubMed: 33641073
Development of a miRNA-controlled dual-sensing system and its application for targeting miR-21 signaling in tumorigenesis [ Exp Mol Med, 2020, 10.1038/s12276-020-00537-z]	PubMed: 33311703
Inhibition of Sema4D/PlexinB1 Signaling Alleviates Vascular Dysfunction in Diabetic Retinopathy [ EMBO Mol Med, 2020, 7;12(2):e10154]	PubMed: 31943789
SRC Promotes Tamoxifen Resistance in Breast Cancer via Up-Regulating SIRT1 [ Onco Targets Ther, 2020, 13:4635-4647]	PubMed: 32547094

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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