Tirbanibulin

N.º de catálogoS2700 Lote:S270001

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Datos técnicos

Fórmula

C₂₆H₂₉N₃O₃

Peso molecular

431.53

Número CAS

897016-82-9

Solubilidad (25°C)*

In vitro

DMSO

86 mg/mL (199.29 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Agregue los solventes al producto individualmente y en orden.)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml significa ligeramente soluble o insoluble.
* Tenga en cuenta que Selleck prueba la solubilidad de todos los compuestos internamente, y la solubilidad real puede diferir ligeramente de los valores publicados. Esto es normal y se debe a ligeras variaciones entre lotes.
* Envío a temperatura ambiente (Las pruebas de estabilidad demuestran que este producto se puede enviar sin medidas de refrigeración.)

Preparación de soluciones madre

Actividad biológica

Descripción

Tirbanibulin, el primer inhibidor clínico de Src (clase peptidomimética) que se dirige al sitio del sustrato peptídico de Src, con GI50 de 9-60 nM en líneas celulares de cáncer. Fase 2.

Objetivos

Src (HuH7) (Cell-free assay)	Src (PLC/PRF/5) (Cell-free assay)	Src (Hep 3B) (Cell-free assay)	Src (Hep G2) (Cell-free assay)
9 nM(GI50)	13 nM(GI50)	26 nM(GI50)	60 nM(GI50)

In vitro

KX2-391 es un inhibidor de Src que se dirige al bolsillo del sustrato de Src. KX2-391 muestra curvas dosis-respuesta pronunciadas contra Huh7 (GI 50 = 9 nM), PLC/PRF/5 (GI 50 = 13 nM), Hep3B (GI 50 = 26 nM) y HepG2 (GI 50 = 60 nM), cuatro líneas celulares de carcinoma hepatocelular (HCC). Se ha descubierto que KX2-391 inhibe ciertas células de leucemia que son resistentes a los fármacos disponibles comercialmente, como las derivadas de células de leucemia crónica con la mutación T3151. KX2-391 se evalúa en ensayos de crecimiento celular impulsados por Src en células NIH3T3/c-Src527F y SYF/c-Src527F y exhibe GI50 con 23 nM y 39 nM, respectivamente.

In vivo

En modelos animales preclínicos de cáncer, se ha demostrado que el KX2-391 administrado por vía oral inhibe el crecimiento tumoral primario y suprime la metástasis.

Protocolo (de referencia)

Ensayo celular:^{^[1]}	Líneas celulares Huh7, PLC/PRF/5, Hep3B, and HepG2 cell lines Concentraciones 6,564 to 0.012 nM Tiempo de incubación 3 days Método 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.

Ensayo celular:^{^[1]}

Líneas celulares
Huh7, PLC/PRF/5, Hep3B, and HepG2 cell lines
Concentraciones
6,564 to 0.012 nM
Tiempo de incubación
3 days
Método
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.

Referencias

https://pubmed.ncbi.nlm.nih.gov/18979199/
https://pubmed.ncbi.nlm.nih.gov/21852023/

Validación de productos por parte del cliente

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

: Datos de [ , , Front Immunol, 2018, 9:2433 ]

: Datos de [ , , Oncotarget, 2016, 7(31):50027-50042 ]

: Datos de [ , , Acta Pharmacol Sin, 2018, 39(8):1326-1337 ]

Sellecks Tirbanibulin Ha sido citado por 41 Publicaciones

S1PR3-driven positive feedback loop sustains STAT3 activation and keratinocyte hyperproliferation in psoriasis [ Cell Death Dis, 2025, 16(1):31]	PubMed: 39833165
Src/FN1 pathway activation drives tumor cell cluster formation and metastasis in lung cancer: A promising therapeutic target [ Sci Adv, 2025, 11(28):eadv7377]	PubMed: 40632865
Tirbanibulin (KX2-391) analog KX2-361 inhibits botulinum neurotoxin serotype A mediated SNAP-25 cleavage in pre- and post-intoxication models in cells [ Drug Dev Res, 2024, 85(6):e22248]	PubMed: 39166850
Anti-tumor effects of tirbanibulin in squamous cell carcinoma cells are mediated via disruption of tubulin-polymerization [ Arch Dermatol Res, 2024, 316(7):341]	PubMed: 38847867
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

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