Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8825 |
Capmatinib 2HCl.H2O
INCB28060 2HCl.H2O,INC-280 2HCl.H2O,NVP-INC280 2HCl.H2O |
c-Met/HGFR | Tyrosine Kinase/Adaptors |
Capmatinib 2HCl.H2O (NVP-INC280 2HCl.H2O) 是一种具有潜在抗肿瘤活性的原癌基因 c-Met (HGFR) 的口服生物可利用抑制剂。 | |||
T1963 |
Capmatinib
NVP-INC280,INC-280,卡马替尼,INCB28060 |
Apoptosis; c-Met/HGFR | Apoptosis; Tyrosine Kinase/Adaptors |
Capmatinib (INCB28060) 是一种具有口服活性的,选择性的,ATP 竞争性的c-Met 激酶抑制剂,IC50值为0.13 nM。它有效抑制 c-Met 依赖性肿瘤细胞的增殖和迁移,可诱导细胞凋亡,有抗肿瘤活性。 | |||
T8416 |
Capmatinib xHCl
INCB28060,Capmatinib hydrochloride(free base),INC280 |
c-Met/HGFR | Tyrosine Kinase/Adaptors |
Capmatinib xHCl (INCB28060) 是一种有效的、口服活性的、选择性的和 ATP 竞争性 c-Met 激酶抑制剂,有效地阻断体外激酶活性 (IC50 = 0.13 nM) 以及在细胞中的组成型或 HGF 刺激活性(IC50 值范围从 0.3 到1.1纳米)。 | |||
T4260 |
Capmatinib 2HCl
INC-280 2HCl,INCB28060盐酸盐,INCB28060 2HCl |
c-Met/HGFR | Tyrosine Kinase/Adaptors |
Capmatinib 2HCl (INC-280 2HCl) 是一种新型的 ATP 竞争性 c-MET 激酶抑制剂,IC50 为 0.13 nM。它具有皮摩尔酶效,对 c-MET 具有高度特异性,选择性超过 10, 000 倍一大组人类激酶。该抑制剂在 c-MET 依赖性肿瘤细胞系中有效阻断 c-MET 磷酸化和其关键下游效应子的激活。因此,它在体外有效抑制 c-MET 依赖性肿瘤细胞增殖和迁移,并有效诱导细胞凋亡。 | |||
T9582 |
CLEFMA
|
NF-κB | NF-κB |
CLEFMA 是一种姜黄素,抑制肿瘤生长与 NF-κB 调节的抗炎和抗转移作用有关,具有抗肿瘤活性。 | |||
T71382 |
KRC-108
|
Others | Others |
KRC-108 is a multiple kinase inhibitor. KRC-108 is a potent inhibitor of Ron, Flt3 and TrkA as well as c-Met. KRC-108 inhibited oncogenic c-Met M1250T and Y1230D more strongly than wild type c-Met. The anti-proliferative activity of KRC-108 was measured by performing a cytotoxicity assay on a panel of cancer cell lines. The GI(50) values (i.e., 50% inhibition of cell growth) for KRC-108 ranged from 0.01 to 4.22 μM for these cancer cell lines. KRC-108 was also effective for the inhibition of tumo... | |||
T83865 |
HP661
|
Others | Others |
HP661是一种针对线粒体复合物I(也称为NADH脱氢酶)的抑制剂,对复合物I具有选择性,以1 µM的浓度抑制其77.6%,而对复合物III抑制率为28.1%,对复合物II和IV则无抑制作用。HP661特异性降低具有高水平氧化磷酸化作用的人类肺癌细胞H460、NCI H441及对trametinib耐药的A549细胞的生存能力(IC50分别为10.6、29.7和15.1 nM),相较于氧化磷酸化水平低的NCI H358人类肺癌细胞(IC50 >10,000 nM)以及非癌性人类胰腺正常上皮细胞(HPNE)和MRC-5人类胎肺成纤维细胞(两者的IC50均>10,000 nM)。当以每天两次,每次30 mg/kg的剂量给药时,HP661在H460小鼠异种移植模型中减少肿瘤体积,并对trametinib引导的肿瘤生长减少产生加成效应。 | |||
T38263 |
TBK1/IKKε-IN-4
TBK1/IKKε-IN-4 |
Others | Others |
TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1]. TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1].TBK1/IK... |