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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5349 |
SCR-1481B1
麦他替尼胺丁三醇,c-Met inhibitor 2 |
VEGFR; c-Met/HGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
SCR-1481B1 (c-Met inhibitor 2) 能够作用于依赖 Met 激活的癌症,对 VEGFR 具有抑制作用。 | |||
T10655 |
c-Met inhibitor 1
3-[(2-甲基-2H-吲唑-5-基)硫基]-6-(1-甲基-1H-吡唑-4-基)-1,2,4-三唑并[4,3-B]哒嗪 |
c-Met/HGFR | Tyrosine Kinase/Adaptors |
c-Met inhibitor 1 是一种 c-Met 受体信号通路抑制剂,可用于癌症的治疗,包括胶质母细胞瘤、胃癌和胰腺癌。 | |||
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。 | |||
T21312 |
Afatinib
阿法替尼,Afatinib free base,BIBW 2992 |
EGFR; Autophagy | Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Afatinib (BIBW 2992) 是一种不可逆的 EGFR 家族抑制剂,抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。 | |||
T1773 |
Afatinib Dimaleate
马来酸阿法替尼,双马来酸盐阿法替尼,BIBW2992,Afatinib,BIBW 2992MA2,Afatinib (BIBW2992) Dimaleate |
EGFR; HER; Autophagy | Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Afatinib Dimaleate (BIBW 2992MA2) 是一种可口服的苯胺基-喹唑啉衍生物和受体酪氨酸激酶表皮生长因子受体家族的抑制剂,具有抗肿瘤活性。它抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。 | |||
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)。 | |||
T6039 |
TAK-285
TAK285,TAK 285 |
EGFR; MEK; HER; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Tyrosine Kinase/Adaptors |
TAK-285 是一种新型 HER2 和 EGFR(HER1) 双重抑制剂,IC50 分别为 17 和 23 nM。它可穿过血脑屏障,有抗肿瘤活性,对 HER1/2 的选择性是 HER4 的 10 倍以上。 | |||
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。 | |||
T6289 |
Dovitinib
TKI258,多韦替尼,CHIR-258,度维替尼 |
VEGFR; FGFR; FLT; PDGFR; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Dovitinib (CHIR-258) 是一种口服有效的、多靶点的酪氨酸激酶 (RTK) 抑制剂,具有抗肿瘤作用。 | |||
T6479 |
Dovitinib lactate hydrate
Dovitinib (TKI258) Lactate,多韦替尼,Dovitinib Lactate,TKI258 |
VEGFR; FGFR; FLT; PDGFR; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Dovitinib lactate hydrate (TKI258) 是一种多靶点的酪氨酸激酶抑制剂,抑制 FLT3,c-Kit,FGFR1/3,VEGFR1/2/3和 PDGFRα/β的 IC50值分别为 1,2,8/9,10/13/8,27/210 nM。 | |||
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. | |||
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。 | |||
T26379 |
1D-2
1D2,1D 2 |
||
1D-2 is a highly potent and exquisitely selective inhibitor of the c-Met protein kinase. | |||
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。 | |||
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. | |||
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。 | |||
T71636 | Golvatinib tartrate | ||
Golvatinib tartrate is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. | |||
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. | |||
T15808 |
Merestinib dihydrochloride
LY2801653 dihydrochloride |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Merestinib dihydrochloride is an effective and orally bioavailable c-Met inhibitor (Ki=2 nM). It has anti-tumor activities and also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), RO | |||
T14282 |
Amuvatinib hydrochloride
HPK 56 hydrochloride,MP470 hydrochloride |
Others | Others |
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret and is also a DNA repair suppressor through suppression of DNA repai | |||
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... | |||
T6193 |
Dovitinib Dilactic Acid
Dovitinib (TKI-258) Dilactic Acid,TKI258 Dilactic acid |
VEGFR; FGFR; FLT; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Dovitinib Dilactic Acid (Dovitinib(TKI-258) Dilactic Acid) 是 Dovitinib 的双乳酸,是一种多靶点 RTK 抑制剂,主要用于 III 类 (FLT3/c-Kit),IC50 为 1 nM/2 nM,对 IV 类 (FGFR1/ 3) 和 V 类 (VEGFR1-4) RTK,IC50 为 8-13 nM,对 InsR、EGFR、c-Met、EphA2、Tie2、IGFR1 和 HER2 的效力较低。 | |||
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 |
---|---|---|---|
T13108 |
Pamufetinib
H2OL3Q4XRD,4-(2-Fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide,TAS-115 |
VEGFR; c-Met/HGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Pamufetinib (TAS-115) 是VEGFR 和c-Met/HGFR 抑制剂,能够抑制 rVEGFR2 (IC50:30 nM)和 rMET (IC50:32 nM)的活性。 |