GW441756

N.º de catálogoS2891 Lote:S289101

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Datos técnicos

Fórmula

C17H13N3O
Peso molecular 275.3 Número CAS 504433-23-2
Solubilidad (25°C)* In vitro DMSO 25 mg/mL (90.81 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 GW441756 es un potente y selectivo inhibidor de TrkA con una IC50 de 2 nM, con muy poca actividad sobre c-Raf1 y CDK2. Este compuesto produce un aumento relevante de caspasa-3 que conduce a la apoptosis.
Objetivos
TrkA
(Cell-free assay)
2 nM
In vitro

GW441756 puede bloquear específicamente la muerte celular inducida por TrkA de manera dosis-dependiente. Este compuesto puede bloquear la producción de γH2AX mediada por TrkAy la apoptosis en células que sobreexpresan TrkA.

Protocolo (de referencia)

Estudio en animales:

[4]
  • Modelos animales

    Wistar male rats

  • Dosificaciones

    10 mg/kg

  • Administración

    i.p.

Referencias

  • https://pubmed.ncbi.nlm.nih.gov/15013000/
  • http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2679291/
  • https://pubmed.ncbi.nlm.nih.gov/18511888/
  • https://pubmed.ncbi.nlm.nih.gov/32042328/

Validación de productos por parte del cliente

Thermal latency and mechanical allodynia were normalized in the RTXw1 + 4MC group (n= 6). In these mice, thermal hypoalgesia reappeared within 2 days of GW441756 injection (D). GW441756 did not affect mechanical thresholds (E) in the RTXw1 + 4MC group. (F, G) The diagrams show behavioral responses of naïve mice to either gambogic amide (open square, n = 6) or GW441756 (open circle, n =6). Gambogic amide induced mild thermal hyperalgesia within 2 days of injection but GW441756 did not affect thermal latencies (F). Both gambogic amide and GW441756 did not affect mechanical responses. *P < 0.05, **P < 0.01, and ***P < 0.001: paired t-test comparing preinjection vs. postinjection effects. #P < 0.05, ##P < 0.01, and ###P < 0.001: between drugs and saline treatments.

Datos de [ , , Exp Neurol, 2018, 300:87-99 ]

Effect of TrkA inhibitorGW441756 on vorinostat andNGFmediated ERK phosphorylation. A)NS-1 cellswere treatedwith vorinostat (1 and 2.5 μM) andNGF (2.5 ng/mL)with and without GW441756 (1 μM) for 3 h. The blots were probed with anti-pERK.1/2 antibody. Vorinostat mediated activation of ERK1/2 phosphorylation (pErk) was abolished in presence of GW441756. Total ERK levels were checked using ERK 1/2 antibody. B) Bar graph represents the densitometric analysis of immunoblots. X axis represents treatments and Y axis represents the ratio of absolute relative density of pERK to the total ERK. The data sets are the mean ± SE of two biological replicates from two independent experiments (values compared to control vs vorinostat 1 μM and 2.5 μM, vorinostat 1 μM and 2.5 μM Vs GW441756 + vorinostat 1 and 2.5 μM respectively). *P < 0.05, **P < 0.001, ***P < 0.0001 indicate significant differences and ns indicates non-significant difference.

Datos de [ , , Mol Cell Neurosci, 2016, 77:11-20. ]

Neurite extension of PC12 cells was visualized by immunostaining (×200 magnification; scale bar, 50 µm) with anti-neurofilament H antibody (red) and nuclei were stained with DAPI (blue). SCDC2 cells (2×104 cells) and rat pheochromocytoma cells PC12 (1×104 cells) were co-cultured and treated with or without TGF-β1 (10 ng/ml) for 4 days. Cells were also treated with TGF-β type I receptor inhibitor SB-431542 (10 µM), TrkA inhibitor GW441756 (2 nM), IL-1β (10 ng/ml), or TNF-α (10 ng/ml) from the beginning of the co-culture. In addition, ATPγS (100 µM) was added to all cultures during cell seeding. Dimethyl sulfoxide was added to cell cultures as a vehicle control for SB-431542 and GW441756, respectively.

Datos de [ , , Int J Mol Med, 2018, 42(3):1484-1494 ]

Sellecks GW441756 Ha sido citado por 20 Publicaciones

Nociceptor neurons promote PDAC progression and cancer pain by interaction with cancer-associated fibroblasts and suppression of natural killer cells [ Cell Res, 2025, 10.1038/s41422-025-01098-4] PubMed: 40122998
Neuronal FSTL4 negatively regulates BDNF-mediated neuron-glioma interaction [ Neurochem Int, 2025, 191:106072] PubMed: 41082941
Androgens and NGF Mediate the Neurite-Outgrowth through Inactivation of RhoA [ Cells, 2023, 12(3)373] PubMed: 36766714
Androgens and NGF Mediate the Neurite-Outgrowth through Inactivation of RhoA. Cells 2023, 12, 373 [ Cells, 2023, 12(3):373] PubMed: None
The effect of Banxia-houpo decoction on CUMS-induced depression by promoting M2 microglia polarization via TrkA/Akt signalling [ J Cell Mol Med, 2023, 10.1111/jcmm.17906] PubMed: 37581474
Huntingtin-associated protein 1 ameliorates neurological function rehabilitation by facilitating neurite elongation through TrKA-MAPK pathway in mice spinal cord injury [ Front Mol Neurosci, 2023, 16:1214150] PubMed: 37609072
Wogonin, a Bioactive Ingredient from Huangqi Guizhi Formula, Alleviates Discogenic Low Back Pain via Suppressing the Overexpressed NGF in Intervertebral Discs [ Mediators Inflamm, 2023, 2023:4436587] PubMed: 36860203
Propionibacterium acnes contributes to low back pain via upregulation of NGF in TLR2-NF-κB/JNK or ROS pathway [ Microbes Infect, 2022, S1286-4579(22)00050-8] PubMed: 35430372
Sea urchin gangliosides exhibit neuritogenic effects in neuronal PC12 cells via TrkA- and TrkB-related pathways [ Biosci Biotechnol Biochem, 2021, 85(3):675-686] PubMed: 33589896
Nerve growth factor activates autophagy in Schwann cells to enhance myelin debris clearance and to expedite nerve regeneration. [ Theranostics, 2020, 10(4):1649-1677] PubMed: 32042328

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