| 名称 | GSK1838705A |
| 描述 | GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases. |
| 细胞实验 | Cells are seeded in 96-well dishes, incubated overnight at 37 °C, and treated with DMSO or GSK1838705A for 72 hours. For the NIH-3T3/LISN proliferation assays, cells are seeded on collagen-coated 96-well tissue culture plates and allowed to adhere for 24 hours. The medium is replaced with serum-free medium and the cells are treated with GSK1838705A for 2 hour. Cells are incubated for 72 hours after addition of IGF-I (30 ng/mL). Cell proliferation is quantified using the CellTiter-Glo Luminescent Cell Viability Assay. IC50s are determined from cytotoxicity curves using a four-parameter curve fit software package (XLfit4(Only for Reference) |
| 激酶实验 | Kinase Assays: Baculovirus-expressed glutathione S-transferase-tagged proteins encoding the intracellular domain of IGF-1R (amino acids 957-1367) and IR (amino acids 979-1382) are used for determinations of IC50s by a homogeneous time-resolved fluorescence assay. A filter binding assay is used for appKi determinations using activated IGF-1R and IR kinases. Expanded kinase-selectivity profiling of GSK1838705A is carried out by screening the compound in the KinaseProfiler panel. |
| 体外活性 | 在负荷COLO 205肿瘤的小鼠体内,GSK1838705A（30 mg/kg）可抑制80%的肿瘤生长.此外,在负荷HT29异种移植物或BxPC3异种移植物的小鼠体内,GSK1838705A也具有抗肿瘤作用.在负荷NIH-3T3/LISN肿瘤的小鼠体内,GSK1838705A（60 mg/kg,p.o.）抑制77%肿瘤生长,且体重无明显损失.在小鼠体内,通过抑制IR信号,GSK1838705A（60 mg/kg）可使血糖水平短暂增加2倍.GSK1838705A（60 mg/kg）抑制已建立的Karpas-299异种移植物的生长（93%）,但不影响大鼠体重. |
| 体内活性 | GSK1838705A可有效抑制细胞中配体诱导的IGF-1R（IC50：85 nM）和IR（IC50：79 nM）磷酸化。GSK1838705A对一系列衍生自固体和血液肿瘤的细胞系,比如L-82/SUP-M2/SK-ES/MCF-7（EC50：24/28/141/203 nM）细胞均有显著抗增殖作用。GSK1838705A可使MCF-7 和NCl-H929细胞在细胞周期的G1 (2N)期积累。GSK1838705A对ALK也有抑制效果（Ki：0.35 nM）,还抑制核仁磷酸蛋白(NPM)-ALK融合细胞的增殖（EC50：24-88 nM）。GSK1838705A对Karpas-299和SR-786细胞中的NPM-ALK磷酸化有显著抑制作用,但对STAT3磷酸化效果一般。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : < 10 mg/mL (18.78 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 100 mg/mL (187.77 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (18.78 mM), Solution.
|
| 关键字 | S6Kinase | S6 Kinase | RSK1 | JNK3 | Insulin Receptor | Inhibitor | inhibit | IGF-1R | IGF1R | GSK-1838705A | GSK1838705A | Cluster of differentiation 246 | CD246 | Anaplastic lymphoma kinase (ALK) | Anaplastic lymphoma kinase | ALK tyrosine kinase receptor | ALK |
| 相关产品 | Astragaloside IV | Berberine hydrogen sulphate | Tranexamic acid | Chloranil | Semaglutide | Sorbic acid | Insulin (human) | Chloramphenicol | L-Cysteine hydrochloride hydrate | Berberine sulfate | Ornithine-α-ketoglutarate | Metacetamol |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 激酶抑制剂库 | 抗纤维化化合物库 | 抗衰老化合物库 | 免疫/炎症分子化合物库 | 神经退行性疾病化合物库 | 膜蛋白靶向化合物库 | 酪氨酸激酶分子库 | 疼痛相关化合物库 |