c-Met

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研究领域

抑制剂选择性比较

c-Met产品

所有产品 c-Met抑制剂(35)

目录号	产品描述	文献引用	实验数据
S1068	Crizotinib (PF-02341066) Crizotinib (PF-02341066) 克唑替尼是一种有效的c-Met和ALK抑制剂，在细胞试验中IC50分别为11 nM 和 24 nM。它同时也是有效的ROS1抑制剂，其Ki值小于0.025 nM。Crizotinib可在多种肺癌细胞系中通过抑制STAT3通路来诱导自噬。	Cancer Cell, 2020, 13;37(1):104-122e12 Nat Commun, 2020, 25;11(1):1556 Sci Adv, 2020, 22;6(21):eaaz8521	(c) Western blot analyses of p-Akt (Ser473) and p-S6RP (Ser235 and Ser236) in two RCT-E565 transplanted tumors treated with vehicle or PF02341066. Samples were isolated 4 h after the last dose from mice treated with PF02341066 for 3 d. (d) Responses of RCT-E565 transplanted tumors in athymic mice to PF02341066 or vehicle. Data are means ±s.e.m. (each group, n = 6). P < 0.005, *P < 0.001 (Student^,s t test).
S1119	Cabozantinib (BMS-907351) Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂，在无细胞试验中IC50为0.035 nM，也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL，IC50分别为1.3 nM，4 nM，4.6 nM，12 nM/11.3 nM/6 nM，14.3 nM 和 7 nM。Cabozantinib 在结肠癌细胞中可通过AKT/GSK-3β/NF-κB信号通路诱导PUMA依赖的凋亡。	Nat Commun, 2020, 1;11(1):2124 Sci Adv, 2020, 22;6(21):eaaz8521 Cell Syst, 2020, 10(3):240-253	Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
S1111	Foretinib (GSK1363089) Foretinib (GSK1363089)是一种ATP竞争性的HGFR和VEGFR抑制剂，对Met和KDR作用最强，在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron， Flt-1/3/4， Kit， PDGFRα/β和Tie-2作用效果稍弱，对FGFR1和EGFR几乎没有抑制活性。Phase 2。	Sci Adv, 2020, 22;6(21):eaaz8521 Genome Med, 2020, 18;12(1):17 Transl Oncol, 2020, 13(2):355-364	c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. Cell growth was determined using the sulforhodamine B assay. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, and TAE-684I. The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
S1070	PHA-665752 PHA-665752是一种有效的，选择性的，ATP竞争性c-Met抑制剂，在无细胞试验中IC50为9 nM，对c-Met的选择性比对 RTKs和 STKs高50倍以上。	Arch Biochem Biophys, 2020, 680:108239 Int J Mol Sci, 2020, 21(2) Nat Commun, 2019, 10(1):3708	A, representative Western blot analyses of samples obtained from NSCLC cells exposed to 1 umol/L erlotinib or PHA-665,752 for 6 hours. Levels of total and phosphorylated forms of EGFR, MET, and HER3. B, representative Western blot analyses of samples obtained as described in A showing the levels of EGFR downstream signaling mediators. Protein samples obtained from untreated and treated cells were separated by SDS-PAGE and immunoblotted with each antibody. Tubulin served to ensure equal loading.
S1080	SU11274 SU11274是一种选择性Met抑制剂，在无细胞试验中IC50为10 nM，对PGDFRβ，EGFR和Tie2没有作用。	J Biol Chem, 2020, 23 pii: jbc Cell Death Dis, 2019, 10(2):139 J Mol Biol, 2019, 431(10):2020-2039	Effect of crizotinib, tivantinib, and SU11274 on levels of c-MET phosphorylation and downstream signaling pathway in SW1736 and TL3 thyroid cancer cells. Cells were prestarved in culture medium containing 0.5% FBS (24 hour) ?either crizotinib or tivantinib (0.1, 1.0, and 10 umol/L) or SU11274 (10 umol/L), and stimulated with 20 ng/mL recombinant human HGF for 10 minutes before lysates were made for Western blotting. A series of c-MET downstream signaling pathway proteins and phosphor proteins were detected using Western blotting. β-Actin was used as a loading balance control.
S6762^New	Bozitinib (PLB-1001) Bozitinib is a highly selective ATP-competitive small-molecule c-Met inhibitor with blood-brain barrier permeability.
S6764^New	TAS-115 TAS-115 is a unique VEGFR/MET-targeted inhibitor with IC50 of 30nM and 32nM for rVEGFR2 and rMET, respectively.
S8854^New	JNJ-38877618(OMO-1) JNJ-38877618 (OMO-1)是一种有效的、高选择性的、具有口服生物利用度的MET kinase抑制剂，Kd值为1.4 nM。其抑制野生型MET和突变型MET(M1268T)的IC50值分别为2 nM和3 nM。
S8676^New	Glumetinib (SCC244) Glumetinib (SCC244)是一种有效的、具有高度选择性的c-Met抑制剂，IC50为0.42 ± 0.02 nmol/L。SCC244对c-Met的选择性比对其他312种所检测激酶（包括RON、Axl、Mer和TyrO3）高2400倍以上。
S6412^New	Altiratinib Altiratinib是有效的TRK, MET, TIE2和VEGFR2激酶抑制剂，对TRKA, B和C的IC50分别为0.9 nM, 4.6 nM和0.8 nM。它抑制MET和MET突变体的IC50范围为0.3-6 nM。
S1112	SGX-523 SGX-523是一种选择性的Met抑制剂，IC50为4 nM，对BRAFV599E， c-Raf， Abl和p38α无抑制活性。Phase 1。	J Pathol, 2020, 250(2):205-216 Acta Pharmacol Sin, 2020, 10.1038/s41401-019-0336-3 Nat Commun, 2019, 10(1):2701	Association of c-Met phosphorylation and s-Met generation in EBC-1 xenograft tumor. Mice were treated with SGX523 at 10 mg/kg, 3 mg/kg, 0.1 mg/kg, at 0 h and 8 h point, respectively. Plasma and tumor lysates were collected using the method described in "Materials and methods"section at 24 h time point. The bar and line in the figure represents the average phosphorylation rate of c-Met and s-Met in subgroups, respectively. Each subgroup consists of four mice with tumor volume around 600 mm³.
S1561	BMS-777607 BMS-777607是一种Met相关的抑制剂，作用于c-Met，Axl，Ron和Tyro3，在无细胞试验中IC50分别为3.9 nM，1.1 nM，1.8 nM和4.3 nM，作用于Met相关靶点比作用于Lck， VEGFR-2，和TrkA/B选择性高40倍，比作用于其他受体和非受体激酶选择性高500多倍。Phase 1/2。	Cell Metab, 2020, 4;31(2):406-421 e7 Front Oncol, 2020, 12;10:700 Cancer Commun (Lond), 2020, 11	Numbers of clonogenic cells from L3.6pl cells and CSCs^＋24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%.
S2753	Tivantinib (ARQ 197) Tivantinib (ARQ 197)是第一个非ATP竞争性的c-Met抑制剂，在无细胞试验中K_i为0.355 μM，对Ron几乎没有作用活性，对EGFR， InsR， PDGFRα和FGFR1/4没有抑制作用。Phase 3。	Sci Adv, 2020, 22;6(21):eaaz8521 Am J Cancer Res, 2020, 1;10(2):564-571 eCollection 2020 Arch Biochem Biophys, 2020, 680:108239	Effect of tivantinib on the mitotic index was compared with the antimitotic drugs paclitaxel and vinblastine after overnight treatment of the HLE cell line with two different concentrations of each drug
S1114	JNJ-38877605 JNJ-38877605是一种ATP竞争性的c-Met抑制剂，IC50为4 nM，作用于c-Met比作用于200种其他酪氨酸和丝-苏氨酸激酶选择性高600倍。Phase 1。	Cell Rep, 2020, 30(10):3383-3396 Cell Death Dis, 2020, 11(2):111 Acta Pharmacol Sin, 2020, 10.1038/s41401-019-0336-3	Growth factors induced ERK phosphorylation in RPE50 and ARPE19. (B) RPE50 cells were untreated (-), treated with 50 nM of HGF or EGF or 50 ng/ml HB-EGF coupled with DMSO or various inhibitors as indicated for 0.5 h.
S1094	PF-04217903 PF-04217903是一种选择性的，ATP竞争性c-Met抑制剂，在A549细胞中IC50为4.8 nM，对致癌基因突变型敏感(对Y1230C突变型没有活性)。Phase 1。	Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.06.003 Neoplasia, 2019, 22(1):1-9 Sci Rep, 2019, 9(1):606	Clonogenicity of LXFA 526L and LXFA 1647L with titration of the MET inhibitor PF-04217903 and combination of PF-04217903 at 0.1 uM with 0.66 uM cetuximab.
S1244	Amuvatinib (MP-470) Amuvatinib (MP-470)是一种有效的，作用于c-Kit、PDGFα和Flt3的多靶点抑制剂，IC50分别为10 nM、40 nM和81 nM。Amuvatinib 可抑制c-MET和c-RET。Amuvatinib 还具有DNA修复蛋白Rad51抑制剂及抗肿瘤的活性。Phase 2。	Oncotarget, 2016, 7(15):19620-30 J Pathol, 2015, 237(1):14-24 Cancer Res, 2014, 74(20):5878-90	Inactivation of AXL by MP470 reverses epithelial to mesenchymal transition. Immunoblot analyses of lysates from TGFβ/TNFα- treated MCF10A cells treated with varying amounts of MP470 for 72 hours.
S1361	MGCD-265 analog MGCD-265是一种有效的，多靶点，及ATP竞争性的c-Met和VEGFR1/2/3抑制剂，IC50分别为1 nM， 3 nM/3 nM/4 nM，也抑制Ron和Tie2。Phase 1/2。	Protein Cell, 2019, 10(3):161-177 Mol Cancer Ther, 2018, 17(7):1526-1539 PLoS One, 2018, 13(4):e0194730	c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, TAE-684, and RON inhibitor I. Columns, means; bars, SEMs (n = 3). The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
S2788	Capmatinib (INCB28060) Capmatinib (INCB28060)是一种新型的，ATP竞争性c-MET抑制剂，无细胞试验中IC50为0.13 nM，对RONβ，EGFR和HER-3无活性。Capmatinib (INCB28060)可抑制 Wnt/β-catenin 和 EMT 信号通路并诱导c-MET扩增阳性的弥漫性胃癌中的凋亡。Phase 1。	Nat Commun, 2020, 25;11(1):1556 Genome Med, 2020, 18;12(1):17 Clin Cancer Res, 2020, 26(6):1408-1419	(a) MET inhibition by INCB28060 prevents HGF-induced MET phosphorylation in MDA-MB231 and HCC-1954 cells. After one hour preincubation with INC2B8060, BC cells were stimulated with HGF for one hour. Phosphorylation of MET and total MET were determined by western blot and quantified by densitometric analysis. Results are expressed as percentage of unstimulated and untreated cells (negative control).
S1124	BMS-754807 BMS-754807是一种有效的IGF-1R/InsR可逆性抑制剂，在无细胞试验中IC50为1.8 nM/1.7 nM，对Met，Aurora A/B，TrkA/B和Ron作用稍弱，对Flt3， Lck，MK2，PKA，PKC等几乎没有抑制活性。Phase 2。	Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2485 Sci Signal, 2020, 26;13(633):eaba3176 Cancers (Basel), 2020, 27;12(5)pii: E1087
S2201	BMS-794833 BMS-794833是一种有效的，ATP竞争性Met/VEGFR2抑制剂，IC50为1.7 nM/15 nM，也抑制Ron， Axl和Flt3，IC50低于3 nM；是BMS-817378的前体药物。 Phase 1。
S1316	AMG-208 AMG-208是一种高度选择性的c-Met抑制剂，IC50为9 nM。Phase 1。
S2774	MK-2461 MK-2461是一种有效的，多靶点抑制剂，作用于c-Met(WT/mutants)，IC50为0.4-2.5 nM，对Ron，和Flt1作用效果稍弱；作用于c-Met比作用于FGFR1， FGFR2， FGFR3， PDGFRβ， KDR， Flt3， Flt4， TrkA和TrkB选择性高8到30倍。Phase 1/2。	Mol Cell Biochem, 2018, 449(1-2):1-8	Both V-H cells and V-J cells are treated with MK-2461, XL-184 or ABT-869, respectively. (i-k) Western blot analysis of sFlt-1 expression after incubation with three VEGF-A receptor inhibitors or in the control.
S4001	Cabozantinib malate (XL184) Cabozantinib malate (XL184)是Cabozantinib的苹果酸盐，是有效的VEGFR2抑制剂，IC50为0.035 nM，也抑制c-Met， Ret， Kit， Flt-1/3/4， Tie2和AXL，无细胞试验中IC50分别为1.3 nM， 4 nM， 4.6 nM， 12 nM/11.3 nM/6 nM， 14.3 nM和7 nM。Cabozantinib malate (XL184)可诱导细胞凋亡。	Sci Adv, 2020, 22;6(21):eaaz8521 Clin Cancer Res, 2020, 20 pii: clincanres Clin Cancer Res, 2020, 8	Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
S2859	Golvatinib (E7050) Golvatinib (E7050)是c-Met和VEGFR-2双重抑制剂，IC50分别为14 nM和16 nM，不抑制bFGF刺激的HUVEC生长(浓度高达1000 nM)。Phase 1/2。	Cell, 2019, 178(6):1478-1492 Cancer Sci, 2017, 108(7):1378-1385 Mol Cancer Ther, 2017, 16(3):506-515	PC-9/LMC-GR cells (2 × 105 cells/well) were incubated in 6-well plates with various concentrations of gefitinib with or without crizotinib (1 μmol/L) or golvatinib (1 μmol/L) for 1 hour. Cell lysate were obtained and subjected to immunoblotting with antibodies toward the indicated molecules.
S2747	AMG-458 AMG-458是一种有效的c-Met抑制剂，K_i为1.2 nM，作用于c-Met比作用于VEGFR2选择性高350倍左右。
S2761	NVP-BVU972 NVP-BVU972是一种有效的，选择性的Met抑制剂，IC50为14 nM。
S7067	Tepotinib (EMD 1214063) Tepotinib (EMD 1214063)是一种有效的，选择性的c-Met抑制剂，IC50为4 nM，作用于c-Met比作用于IRAK4， TrkA， Axl， IRAK1和Mer选择性高200倍以上。Tepotinib 可诱导自噬。Phase 1。	Virology, 2019, 531:57-68 J Thorac Oncol, 2019, 14(10):1753-1765 Biochim Biophys Acta Mol Basis Dis, 2018, 1864(3):793-803	Ectopic expression of a RNAi-resistant SMARCE1 cDNA resensitizes SMARCE1-knockdown cells to MET inhibition in MET-amplified NSCLC cells. The above-described cells were grown in the absence or presence of 300 nM Crizotinib, 150 nM EMD1214063, or 150 nM PHA665752. Cells were then fixed, stained and photographed after 12 days (untreated) or 28 days (treated).
S8167	AMG 337 AMG 337是一种口服的、ATP竞争性的、高度选择性MET 受体抑制剂。IC50为1 nM。	Cancer Cell, 2019, 36(1):35-50
S7014	Merestinib (LY2801653) Merestinib (LY2801653) 是一种2型ATP竞争型的慢抑制剂，抑制MET酪氨酸激酶，Ki值为2 nM。药效的停留时间为0.00132 min(-1)，t_^1/2为525 min。Merestinib (LY2801653) 还可抑制MST1R、AXL、ROS1、MKNK1/2、FLT3、MERTK、DDR1和DDR2，其对应的IC50值分别为11 nM、2 nM、23 nM、7 nM、7 nM、10 nM、0.1 nM 和 7 nM。	Front Oncol, 2020, 12;10:700 Cancer Commun (Lond), 2020, 11 J Thorac Oncol, 2019, 14(10):1753-1765
S8404	S49076 S49076是一种新型的、有效的MET, AXL/MER和FGFR1/2/3抑制剂，IC50低于20 nM。	Mol Brain, 2020, 4;13(1):66
S9308	Pulsatilla saponin D Pulsatilla saponin D, isolated from the root of Pulsatilla koreana, targets c-Met and exerts antiangiogenic and antitumor activities.
S7564	SAR125844 SAR125844是一种有效的、高选择性的MET激酶抑制剂，对野生型MET激酶具有纳摩尔级活性（IC50=4.2 nM），对H1094Y, Y1235D, M1250T, L1195V和D1228H突变体的IC50分别为0.22, 1.7, 6.5, 65和81 nM。
S3759	Norcantharidin Norcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
S7669	NPS-1034 NPS-1034是一种双Met/Axl抑制剂，IC50分别为48 nM和10.3 nM。
S7674	Savolitinib(AZD6094) Savolitinib (volitinib, AZD6094, HMPL-504)是新型的、有效的、选择性的MET抑制剂，在对多种病例迹象中进行临床研发，如乳头状肾细胞癌。其对c-Met和p-Met的IC50分别为5 nM和3 nM。相对于所检测的274种激酶，Savolitinib对c-Met具有精确的选择性。	Nature, 2020, 580(7801):136-141 Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-3608 Biomolecules, 2020, 10(2)
S5115	Sodium L-ascorbyl-2-phosphate Sodium L-ascorbyl-2-phosphate (Sodium ascorbyl phosphate, SAP) is specifically produced for use as a stabilized source of vitamin C in cosmetic products. It is used in skin care recipes for UV protection, collagen production, as an antioxidant and for its skin lightening and brightening effects.

目录号	产品描述	文献引用	实验数据
S1068	Crizotinib (PF-02341066) Crizotinib (PF-02341066) 克唑替尼是一种有效的c-Met和ALK抑制剂，在细胞试验中IC50分别为11 nM 和 24 nM。它同时也是有效的ROS1抑制剂，其Ki值小于0.025 nM。Crizotinib可在多种肺癌细胞系中通过抑制STAT3通路来诱导自噬。	Cancer Cell,2020, 13;37(1):104-122e12 Nat Commun,2020, 25;11(1):1556 Sci Adv,2020, 22;6(21):eaaz8521	(c) Western blot analyses of p-Akt (Ser473) and p-S6RP (Ser235 and Ser236) in two RCT-E565 transplanted tumors treated with vehicle or PF02341066. Samples were isolated 4 h after the last dose from mice treated with PF02341066 for 3 d. (d) Responses of RCT-E565 transplanted tumors in athymic mice to PF02341066 or vehicle. Data are means ±s.e.m. (each group, n = 6). P < 0.005, *P < 0.001 (Student^,s t test).
S1119	Cabozantinib (BMS-907351) Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂，在无细胞试验中IC50为0.035 nM，也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL，IC50分别为1.3 nM，4 nM，4.6 nM，12 nM/11.3 nM/6 nM，14.3 nM 和 7 nM。Cabozantinib 在结肠癌细胞中可通过AKT/GSK-3β/NF-κB信号通路诱导PUMA依赖的凋亡。	Nat Commun,2020, 1;11(1):2124 Sci Adv,2020, 22;6(21):eaaz8521 Cell Syst,2020, 10(3):240-253	Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
S1111	Foretinib (GSK1363089) Foretinib (GSK1363089)是一种ATP竞争性的HGFR和VEGFR抑制剂，对Met和KDR作用最强，在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron， Flt-1/3/4， Kit， PDGFRα/β和Tie-2作用效果稍弱，对FGFR1和EGFR几乎没有抑制活性。Phase 2。	Sci Adv,2020, 22;6(21):eaaz8521 Genome Med,2020, 18;12(1):17 Transl Oncol,2020, 13(2):355-364	c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. Cell growth was determined using the sulforhodamine B assay. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, and TAE-684I. The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
S1070	PHA-665752 PHA-665752是一种有效的，选择性的，ATP竞争性c-Met抑制剂，在无细胞试验中IC50为9 nM，对c-Met的选择性比对 RTKs和 STKs高50倍以上。	Arch Biochem Biophys,2020, 680:108239 Int J Mol Sci,2020, 21(2) Nat Commun,2019, 10(1):3708	A, representative Western blot analyses of samples obtained from NSCLC cells exposed to 1 umol/L erlotinib or PHA-665,752 for 6 hours. Levels of total and phosphorylated forms of EGFR, MET, and HER3. B, representative Western blot analyses of samples obtained as described in A showing the levels of EGFR downstream signaling mediators. Protein samples obtained from untreated and treated cells were separated by SDS-PAGE and immunoblotted with each antibody. Tubulin served to ensure equal loading.
S1080	SU11274 SU11274是一种选择性Met抑制剂，在无细胞试验中IC50为10 nM，对PGDFRβ，EGFR和Tie2没有作用。	J Biol Chem,2020, 23 pii: jbc Cell Death Dis,2019, 10(2):139 J Mol Biol,2019, 431(10):2020-2039	Effect of crizotinib, tivantinib, and SU11274 on levels of c-MET phosphorylation and downstream signaling pathway in SW1736 and TL3 thyroid cancer cells. Cells were prestarved in culture medium containing 0.5% FBS (24 hour) ?either crizotinib or tivantinib (0.1, 1.0, and 10 umol/L) or SU11274 (10 umol/L), and stimulated with 20 ng/mL recombinant human HGF for 10 minutes before lysates were made for Western blotting. A series of c-MET downstream signaling pathway proteins and phosphor proteins were detected using Western blotting. β-Actin was used as a loading balance control.
S6762^New	Bozitinib (PLB-1001) Bozitinib is a highly selective ATP-competitive small-molecule c-Met inhibitor with blood-brain barrier permeability.
S6764^New	TAS-115 TAS-115 is a unique VEGFR/MET-targeted inhibitor with IC50 of 30nM and 32nM for rVEGFR2 and rMET, respectively.
S8854^New	JNJ-38877618(OMO-1) JNJ-38877618 (OMO-1)是一种有效的、高选择性的、具有口服生物利用度的MET kinase抑制剂，Kd值为1.4 nM。其抑制野生型MET和突变型MET(M1268T)的IC50值分别为2 nM和3 nM。
S8676^New	Glumetinib (SCC244) Glumetinib (SCC244)是一种有效的、具有高度选择性的c-Met抑制剂，IC50为0.42 ± 0.02 nmol/L。SCC244对c-Met的选择性比对其他312种所检测激酶（包括RON、Axl、Mer和TyrO3）高2400倍以上。
S6412^New	Altiratinib Altiratinib是有效的TRK, MET, TIE2和VEGFR2激酶抑制剂，对TRKA, B和C的IC50分别为0.9 nM, 4.6 nM和0.8 nM。它抑制MET和MET突变体的IC50范围为0.3-6 nM。
S1112	SGX-523 SGX-523是一种选择性的Met抑制剂，IC50为4 nM，对BRAFV599E， c-Raf， Abl和p38α无抑制活性。Phase 1。	J Pathol,2020, 250(2):205-216 Acta Pharmacol Sin,2020, 10.1038/s41401-019-0336-3 Nat Commun,2019, 10(1):2701	Association of c-Met phosphorylation and s-Met generation in EBC-1 xenograft tumor. Mice were treated with SGX523 at 10 mg/kg, 3 mg/kg, 0.1 mg/kg, at 0 h and 8 h point, respectively. Plasma and tumor lysates were collected using the method described in "Materials and methods"section at 24 h time point. The bar and line in the figure represents the average phosphorylation rate of c-Met and s-Met in subgroups, respectively. Each subgroup consists of four mice with tumor volume around 600 mm³.
S1561	BMS-777607 BMS-777607是一种Met相关的抑制剂，作用于c-Met，Axl，Ron和Tyro3，在无细胞试验中IC50分别为3.9 nM，1.1 nM，1.8 nM和4.3 nM，作用于Met相关靶点比作用于Lck， VEGFR-2，和TrkA/B选择性高40倍，比作用于其他受体和非受体激酶选择性高500多倍。Phase 1/2。	Cell Metab,2020, 4;31(2):406-421 e7 Front Oncol,2020, 12;10:700 Cancer Commun (Lond),2020, 11	Numbers of clonogenic cells from L3.6pl cells and CSCs^＋24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%.
S2753	Tivantinib (ARQ 197) Tivantinib (ARQ 197)是第一个非ATP竞争性的c-Met抑制剂，在无细胞试验中K_i为0.355 μM，对Ron几乎没有作用活性，对EGFR， InsR， PDGFRα和FGFR1/4没有抑制作用。Phase 3。	Sci Adv,2020, 22;6(21):eaaz8521 Am J Cancer Res,2020, 1;10(2):564-571 eCollection 2020 Arch Biochem Biophys,2020, 680:108239	Effect of tivantinib on the mitotic index was compared with the antimitotic drugs paclitaxel and vinblastine after overnight treatment of the HLE cell line with two different concentrations of each drug
S1114	JNJ-38877605 JNJ-38877605是一种ATP竞争性的c-Met抑制剂，IC50为4 nM，作用于c-Met比作用于200种其他酪氨酸和丝-苏氨酸激酶选择性高600倍。Phase 1。	Cell Rep,2020, 30(10):3383-3396 Cell Death Dis,2020, 11(2):111 Acta Pharmacol Sin,2020, 10.1038/s41401-019-0336-3	Growth factors induced ERK phosphorylation in RPE50 and ARPE19. (B) RPE50 cells were untreated (-), treated with 50 nM of HGF or EGF or 50 ng/ml HB-EGF coupled with DMSO or various inhibitors as indicated for 0.5 h.
S1094	PF-04217903 PF-04217903是一种选择性的，ATP竞争性c-Met抑制剂，在A549细胞中IC50为4.8 nM，对致癌基因突变型敏感(对Y1230C突变型没有活性)。Phase 1。	Cell Chem Biol,2019, 10.1016/j.chembiol.2019.06.003 Neoplasia,2019, 22(1):1-9 Sci Rep,2019, 9(1):606	Clonogenicity of LXFA 526L and LXFA 1647L with titration of the MET inhibitor PF-04217903 and combination of PF-04217903 at 0.1 uM with 0.66 uM cetuximab.
S1244	Amuvatinib (MP-470) Amuvatinib (MP-470)是一种有效的，作用于c-Kit、PDGFα和Flt3的多靶点抑制剂，IC50分别为10 nM、40 nM和81 nM。Amuvatinib 可抑制c-MET和c-RET。Amuvatinib 还具有DNA修复蛋白Rad51抑制剂及抗肿瘤的活性。Phase 2。	Oncotarget,2016, 7(15):19620-30 J Pathol,2015, 237(1):14-24 Cancer Res,2014, 74(20):5878-90	Inactivation of AXL by MP470 reverses epithelial to mesenchymal transition. Immunoblot analyses of lysates from TGFβ/TNFα- treated MCF10A cells treated with varying amounts of MP470 for 72 hours.
S1361	MGCD-265 analog MGCD-265是一种有效的，多靶点，及ATP竞争性的c-Met和VEGFR1/2/3抑制剂，IC50分别为1 nM， 3 nM/3 nM/4 nM，也抑制Ron和Tie2。Phase 1/2。	Protein Cell,2019, 10(3):161-177 Mol Cancer Ther,2018, 17(7):1526-1539 PLoS One,2018, 13(4):e0194730	c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, TAE-684, and RON inhibitor I. Columns, means; bars, SEMs (n = 3). The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
S2788	Capmatinib (INCB28060) Capmatinib (INCB28060)是一种新型的，ATP竞争性c-MET抑制剂，无细胞试验中IC50为0.13 nM，对RONβ，EGFR和HER-3无活性。Capmatinib (INCB28060)可抑制 Wnt/β-catenin 和 EMT 信号通路并诱导c-MET扩增阳性的弥漫性胃癌中的凋亡。Phase 1。	Nat Commun,2020, 25;11(1):1556 Genome Med,2020, 18;12(1):17 Clin Cancer Res,2020, 26(6):1408-1419	(a) MET inhibition by INCB28060 prevents HGF-induced MET phosphorylation in MDA-MB231 and HCC-1954 cells. After one hour preincubation with INC2B8060, BC cells were stimulated with HGF for one hour. Phosphorylation of MET and total MET were determined by western blot and quantified by densitometric analysis. Results are expressed as percentage of unstimulated and untreated cells (negative control).
S1124	BMS-754807 BMS-754807是一种有效的IGF-1R/InsR可逆性抑制剂，在无细胞试验中IC50为1.8 nM/1.7 nM，对Met，Aurora A/B，TrkA/B和Ron作用稍弱，对Flt3， Lck，MK2，PKA，PKC等几乎没有抑制活性。Phase 2。	Clin Cancer Res,2020, 10.1158/1078-0432.CCR-19-2485 Sci Signal,2020, 26;13(633):eaba3176 Cancers (Basel),2020, 27;12(5)pii: E1087
S2201	BMS-794833 BMS-794833是一种有效的，ATP竞争性Met/VEGFR2抑制剂，IC50为1.7 nM/15 nM，也抑制Ron， Axl和Flt3，IC50低于3 nM；是BMS-817378的前体药物。 Phase 1。
S1316	AMG-208 AMG-208是一种高度选择性的c-Met抑制剂，IC50为9 nM。Phase 1。
S2774	MK-2461 MK-2461是一种有效的，多靶点抑制剂，作用于c-Met(WT/mutants)，IC50为0.4-2.5 nM，对Ron，和Flt1作用效果稍弱；作用于c-Met比作用于FGFR1， FGFR2， FGFR3， PDGFRβ， KDR， Flt3， Flt4， TrkA和TrkB选择性高8到30倍。Phase 1/2。	Mol Cell Biochem,2018, 449(1-2):1-8	Both V-H cells and V-J cells are treated with MK-2461, XL-184 or ABT-869, respectively. (i-k) Western blot analysis of sFlt-1 expression after incubation with three VEGF-A receptor inhibitors or in the control.
S4001	Cabozantinib malate (XL184) Cabozantinib malate (XL184)是Cabozantinib的苹果酸盐，是有效的VEGFR2抑制剂，IC50为0.035 nM，也抑制c-Met， Ret， Kit， Flt-1/3/4， Tie2和AXL，无细胞试验中IC50分别为1.3 nM， 4 nM， 4.6 nM， 12 nM/11.3 nM/6 nM， 14.3 nM和7 nM。Cabozantinib malate (XL184)可诱导细胞凋亡。	Sci Adv,2020, 22;6(21):eaaz8521 Clin Cancer Res,2020, 20 pii: clincanres Clin Cancer Res,2020, 8	Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
S2859	Golvatinib (E7050) Golvatinib (E7050)是c-Met和VEGFR-2双重抑制剂，IC50分别为14 nM和16 nM，不抑制bFGF刺激的HUVEC生长(浓度高达1000 nM)。Phase 1/2。	Cell,2019, 178(6):1478-1492 Cancer Sci,2017, 108(7):1378-1385 Mol Cancer Ther,2017, 16(3):506-515	PC-9/LMC-GR cells (2 × 105 cells/well) were incubated in 6-well plates with various concentrations of gefitinib with or without crizotinib (1 μmol/L) or golvatinib (1 μmol/L) for 1 hour. Cell lysate were obtained and subjected to immunoblotting with antibodies toward the indicated molecules.
S2747	AMG-458 AMG-458是一种有效的c-Met抑制剂，K_i为1.2 nM，作用于c-Met比作用于VEGFR2选择性高350倍左右。
S2761	NVP-BVU972 NVP-BVU972是一种有效的，选择性的Met抑制剂，IC50为14 nM。
S7067	Tepotinib (EMD 1214063) Tepotinib (EMD 1214063)是一种有效的，选择性的c-Met抑制剂，IC50为4 nM，作用于c-Met比作用于IRAK4， TrkA， Axl， IRAK1和Mer选择性高200倍以上。Tepotinib 可诱导自噬。Phase 1。	Virology,2019, 531:57-68 J Thorac Oncol,2019, 14(10):1753-1765 Biochim Biophys Acta Mol Basis Dis,2018, 1864(3):793-803	Ectopic expression of a RNAi-resistant SMARCE1 cDNA resensitizes SMARCE1-knockdown cells to MET inhibition in MET-amplified NSCLC cells. The above-described cells were grown in the absence or presence of 300 nM Crizotinib, 150 nM EMD1214063, or 150 nM PHA665752. Cells were then fixed, stained and photographed after 12 days (untreated) or 28 days (treated).
S8167	AMG 337 AMG 337是一种口服的、ATP竞争性的、高度选择性MET 受体抑制剂。IC50为1 nM。	Cancer Cell,2019, 36(1):35-50
S7014	Merestinib (LY2801653) Merestinib (LY2801653) 是一种2型ATP竞争型的慢抑制剂，抑制MET酪氨酸激酶，Ki值为2 nM。药效的停留时间为0.00132 min(-1)，t_^1/2为525 min。Merestinib (LY2801653) 还可抑制MST1R、AXL、ROS1、MKNK1/2、FLT3、MERTK、DDR1和DDR2，其对应的IC50值分别为11 nM、2 nM、23 nM、7 nM、7 nM、10 nM、0.1 nM 和 7 nM。	Front Oncol,2020, 12;10:700 Cancer Commun (Lond),2020, 11 J Thorac Oncol,2019, 14(10):1753-1765
S8404	S49076 S49076是一种新型的、有效的MET, AXL/MER和FGFR1/2/3抑制剂，IC50低于20 nM。	Mol Brain,2020, 4;13(1):66
S9308	Pulsatilla saponin D Pulsatilla saponin D, isolated from the root of Pulsatilla koreana, targets c-Met and exerts antiangiogenic and antitumor activities.
S7564	SAR125844 SAR125844是一种有效的、高选择性的MET激酶抑制剂，对野生型MET激酶具有纳摩尔级活性（IC50=4.2 nM），对H1094Y, Y1235D, M1250T, L1195V和D1228H突变体的IC50分别为0.22, 1.7, 6.5, 65和81 nM。
S3759	Norcantharidin Norcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
S7669	NPS-1034 NPS-1034是一种双Met/Axl抑制剂，IC50分别为48 nM和10.3 nM。
S7674	Savolitinib(AZD6094) Savolitinib (volitinib, AZD6094, HMPL-504)是新型的、有效的、选择性的MET抑制剂，在对多种病例迹象中进行临床研发，如乳头状肾细胞癌。其对c-Met和p-Met的IC50分别为5 nM和3 nM。相对于所检测的274种激酶，Savolitinib对c-Met具有精确的选择性。	Nature,2020, 580(7801):136-141 Clin Cancer Res,2020, 10.1158/1078-0432.CCR-19-3608 Biomolecules,2020, 10(2)

目录号	产品描述	文献引用	实验数据
S5115	Sodium L-ascorbyl-2-phosphate Sodium L-ascorbyl-2-phosphate (Sodium ascorbyl phosphate, SAP) is specifically produced for use as a stabilized source of vitamin C in cosmetic products. It is used in skin care recipes for UV protection, collagen production, as an antioxidant and for its skin lightening and brightening effects.

目录号

产品描述

文献引用

实验数据

S5115

Sodium L-ascorbyl-2-phosphate

Sodium L-ascorbyl-2-phosphate (Sodium ascorbyl phosphate, SAP) is specifically produced for use as a stabilized source of vitamin C in cosmetic products. It is used in skin care recipes for UV protection, collagen production, as an antioxidant and for its skin lightening and brightening effects.

研究领域

产品类型

c-Met

信号通路图

研究领域

抑制剂选择性比较

c-Met产品