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Cat. No. | Product Name | Target | Signaling Pathways |
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T10654 |
c-Met-IN-2
|
c-Met/HGFR | Tyrosine Kinase/Adaptors |
c-Met-IN-2 is a selective and orally available c-Met inhibitor (IC50: 0.6 nM) with antitumor activity. | |||
T13194 |
CSF1R-IN-2
|
c-Fms; c-Met/HGFR; Src | Angiogenesis; Tyrosine Kinase/Adaptors |
CSF1R-IN-2 是一种口服具有活力的、有效的 SRC,MET 和 c-FMS 抑制剂,它们的 IC50 值分别为 0.12 nM,0.14 nM 和 0.76 nM。 | |||
T72759 | c-Met/HDAC-IN-2 | ||
c-Met/HDAC-IN-2 是一种高效的c-Met 和HDAC 双重抑制剂,对HDAC1与c-Met 的IC50分别为 18.49 nM 和 5.40 nM。c-Met/HDAC-IN-2 对几种癌细胞具有抗增殖活性。c-Met/HDAC-IN-2 能将 HCT-116 细胞周期阻滞在 G2/M 期,诱导细胞凋亡 (apoptosis)。c-Met/HDAC-IN-2 可用于抗癌耐药研究。 | |||
T80874 | VEGFR-2/c-Met-IN-1 | VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2/c-Met-IN-1为VEGFR-2及c-Met的双重抑制剂,IC50值为138 nM和74 nM,显示出抗肿瘤活性。 | |||
T3455 |
Merestinib
LY2801653 |
Discoidin Domain Receptor (DDR); FLT; c-Met/HGFR; ROS; ROS Kinase | Angiogenesis; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Merestinib (LY2801653) 是一种有效的口服生物可利用的具有抗肿瘤活性的c-Met 抑制剂。 | |||
T6517 |
Golvatinib
E-7050,戈伐替尼 |
VEGFR; c-Met/HGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Golvatinib (E-7050) 是一种 c-Met (IC50:14 nM) 和 VEGFR2 (IC50:16 nM) 的双重抑制剂。 | |||
T2054 |
Altiratinib
DCC-2701 |
VEGFR; Tie-2; FLT; Trk receptor; c-Met/HGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Altiratinib (DCC-2701) 是一种多靶点激酶抑制剂,能够抑制 MET (IC50:2.7 nM),TIE2 (IC50:8 nM),VEGFR2 (IC50:9.2 nM),FLT3 (IC50:9.3 nM),Trk1 (IC50:0.85 nM),Trk2 (IC50:4.6 nM) 和 Trk3 (IC50:0.83 nM)。 | |||
T2668 |
JNK-IN-8
JNK Inhibitor XVI |
JNK; c-Kit | MAPK; Tyrosine Kinase/Adaptors |
JNK-IN-8 (JNK Inhibitor XVI) 是一种有效的JNK 抑制剂,抑制JNK1、JNK2和JNK3,IC50分别为 4.7、18.7 和 1 nM。 | |||
T63656 | c-Met-IN-11 | ||
c-Met-IN-11 是 c-MET (IC50: 41.4 nM) 和 VEGFR-2 (IC50: 71.1 nM) 的有效抑制剂。 | |||
T28899 |
T-1840383
|
||
T-1840383 is an inhibitor of VEGF-induced VEGFR-2 phosphorylation and HGF-induced c-Met phosphorylation in vascular endothelial cells and cancer epithelial cells. | |||
T71187 |
Foretinib phosphate
|
||
Foretinib phosphate is an orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers. | |||
T71382 |
KRC-108
|
||
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... | |||
T79572 |
MAPK-IN-2
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
MAPK-IN-2 (化合物3h)是一种携带抗肿瘤活性的高效MAPK抑制剂。它在多个癌细胞系中有效抑制了细胞增殖,并对MAPK途径表现出强大的抑制效果(EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, CDK4/6 IC50=95和184 nM),对突变型EGFR和B-RAF亦展现出高效力(EGFRT790M IC50=69 nM, B-RAFV600E IC50=83 nM)。 | |||
T83911 |
CYY292
|
||
CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂(IC50分别为5.35、4.6、28、28和78 nM)。该化合物对这些激酶的选择性高于FGFR4(IC50 > 1,000 nM),但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体(IGF-1R;IC50分别为67、33、36和75 nM),以及EGFR、布鲁顿酪氨酸激酶(BTK)、细胞周期依赖性激酶4(Cdk4)/cyclin D3和MET(IC50分别为128、198、214和396 nM)。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖(IC50分别为0.84、0.76、1.36和0.72 µM)。在0.3和0.5 µM的浓度下,它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292(30 mg/kg)在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5S1331 |
Herbacetin
|
c-Met/HGFR; Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Herbacetin 是一种亚麻籽中的天然类黄酮,具有多种药理活性,如抗氧化、抗炎、抗癌作用。 它是鸟氨酸脱羧酶Ornithine decarboxylase (ODC)变构抑制剂,能够直接与 ODC 上的 Asp44,Asp243 和 Glu384 结合。其中鸟氨酸脱羧酶是多胺生物合成中的限速酶。 |