Tivantinib
别名: ARQ 197
Tivantinib是第一个非ATP竞争性的c-Met抑制剂，在无细胞试验中Ki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。Tivantinib (ARQ 197) 可诱导G2/M期细胞阻滞和凋亡。
Tivantinib Chemical Structure
CAS: 905854-02-6
产品质控
批次：
纯度：
99.65%
99.65
Tivantinib相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| MNK-45 | Kinase assay | ~10 μM | inhibits c-Met phosphorylation and downstream c-Met signaling pathways | 20484018 | |
| HT29 | Kinase assay | ~10 μM | inhibits c-Met phosphorylation and downstream c-Met signaling pathways | 20484018 | |
| MDA-MB-231 | Kinase assay | ~10 μM | inhibits c-Met phosphorylation and downstream c-Met signaling pathways | 20484018 | |
| NCI-H441 | Kinase assay | ~10 μM | inhibits c-Met phosphorylation and downstream c-Met signaling pathways | 20484018 | |
| SK-MEL-28 | Growth inhibitory assay | 33 μM | IC50>33 μM | 20484018 | |
| NCI-H661 | Growth inhibitory assay | 33 μM | IC50>33 μM | 20484018 | |
| NCI-H446 | Growth inhibitory assay | 33 μM | IC50=7 μM | 20484018 | |
| MDA-MB-231 | Growth inhibitory assay | 33 μM | IC50=0.55 μM | 20484018 | |
| DLD-1 | Growth inhibitory assay | 33 μM | IC50=0.53 μM | 20484018 | |
| A549 | Growth inhibitory assay | 33 μM | IC50=0.59 μM | 20484018 | |
| SK-OV-3 | Growth inhibitory assay | 33 μM | IC50=0.66 μM | 20484018 | |
| NCI-H460 | Growth inhibitory assay | 33 μM | IC50=0.6 μM | 20484018 | |
| A375 | Growth inhibitory assay | 33 μM | IC50=0.42 μM | 20484018 | |
| NCI-H441 | Growth inhibitory assay | 33 μM | IC50=0.3 μM | 20484018 | |
| HT29 | Growth inhibitory assay | 33 μM | IC50=0.49 μM | 20484018 | |
| MKN-45 | Growth inhibitory assay | 33 μM | IC50=0.58 μM | 20484018 | |
| HT29 | Apoptosis assay | ~10 μM | significantly induces apoptosis by 80-90%. | 20484018 | |
| MKN-45 | Apoptosis assay | ~10 μM | significantly induces apoptosis by 80-90%. | 20484018 | |
| MDA-MB-231 | Apoptosis assay | ~10 μM | modestly induces apoptosis by 35%. | 20484018 | |
| MDA-MB-231/TGL | Growth inhibitory assay | ~100 μM | GI50=1.2 μM | 22027690 | |
| 1833/TGL | Growth inhibitory assay | ~100 μM | GI50=3.7 μM | 22027690 | |
| EBC1 | Cytotoxic assay | ~10 μM | inhibits the cell growth. | 23598276 | |
| SNU638 | Cytotoxic assay | ~10 μM | inhibits the cell growth. | 23598276 | |
| A549 | Cytotoxic assay | ~10 μM | not affect | 23598276 | |
| H460 | Cytotoxic assay | ~10 μM | not affect | 23598276 | |
| HCC827 | Cytotoxic assay | ~10 μM | not affect | 23598276 | |
| A549 | Function assay | 10 μM | disrupts microtubule | 23598276 | |
| EBC1 | Function assay | 10 μM | disrupts microtubule | 23598276 | |
| H460 | Function assay | 10 μM | inhibits tubulin polymerization | 25313010 | |
| K562/VCR | Cytotoxic assay | ~10 μM | shows cytotoxic activity | 25313010 | |
| CEM/VBL | Cytotoxic assay | ~10 μM | shows cytotoxic activity | 25313010 | |
| U266 | Cytotoxic assay | ~3 μM | IC50=1.1 μM | 25810013 | |
| OPM-2 | Cytotoxic assay | ~3 μM | IC50=1.8 μM | 25810013 | |
| MM.1S | Cytotoxic assay | ~3 μM | IC50=1.6 μM | 25810013 | |
| MM.1R | Growth inhibitory assay | 3 μM | inhibits cell growth by 49% | 25810013 | |
| RPMI-8226 | Cytotoxic assay | ~3 μM | IC50=0.9 μM | 25810013 | |
| ANBL-6 | Cytotoxic assay | 1 μM | induces cell death by more than 50% | 25810013 | |
| ANLB-6/V10R | Cytotoxic assay | 1 μM | induces cell death by more than 50% | 25810013 | |
| KAS-6/1 | Cytotoxic assay | 1 μM | induces cell death by more than 50% | 25810013 | |
| KAS-6/V10R | Cytotoxic assay | 1 μM | induces cell death by more than 50% | 25810013 | |
| KAS-6/R10R | Cytotoxic assay | 1 μM | induces cell death by more than 50% | 25810013 | |
| 8226/S | Growth inhibitory assay | 3 μM | inhibits cell growth by 54% | 25810013 | |
| 8226/LR-5 | Growth inhibitory assay | 3 μM | inhibits cell growth by 54% | 25810013 | |
| Huh7 | Cytotoxic assay | ~4.8 μM | IC50=9.9 nM | 26259250 | |
| Hep3B | Cytotoxic assay | ~4.8 μM | IC50=448.7 nM | 26259250 | |
| HepG2 | Cytotoxic assay | ~4.8 μM | IC50=139.77 nM | 26259250 | |
| Chang | Cytotoxic assay | ~4.8 μM | IC50=448.7 nM | 26259250 | |
| Huh7 | Function assay | 1.6 μM | causes a G2/M cell cycle arrest | 26259250 | |
| Hep3B | Function assay | 1.6 μM | causes a G2/M cell cycle arrest | 26259250 | |
| HepG2 | Function assay | 1.6 μM | causes a G2/M cell cycle arrest | 26259250 | |
| Chang | Function assay | 1.6 μM | causes a G2/M cell cycle arrest | 26259250 | |
| MHCC97L | Growth inhibitory assay | ~10 μM | IC50=315 nM | 26458953 | |
| MHCC97H | Growth inhibitory assay | ~10 μM | IC50=368 nM | 26458953 | |
| Huh7 | Growth inhibitory assay | ~10 μM | IC50=265 nM | 26458953 | |
| HepG2 | Growth inhibitory assay | ~10 μM | IC50=392 nM | 26458953 | |
| MHCC97L | Function assay | 1 μM | induces microtubules depolymerization | 26458953 | |
| Huh7 | Function assay | 1 μM | induces microtubules depolymerization | 26458953 | |
| MHCC97L | Apoptosis assay | 1 μM | induces apoptosis | 26458953 | |
| Huh7 | Apoptosis assay | 1 μM | induces apoptosis | 26458953 | |
| C3H 10T1/2 mouse fibroblasts | Kinase assay | 25 μM | reduces Histone H3 and H4 acetylation levels | 20534345 | |
| H23 | Growth inhibitory assay | 25 μM | significantly inhibits cell growth. | 20534345 | |
| WM35 | Growth inhibitory assay | 10 μM | significantly inhibits cell growth. | 20534345 | |
| NIH 3T3 | Growth inhibitory assay | 10 μM | does not have a significant inhibitory effect | 20534345 | |
| H838 | Growth inhibitory assay | 10 μM | does not have a significant inhibitory effect | 20534345 | |
| H1395 | Growth inhibitory assay | 10 μM | does not have a significant inhibitory effect | 20534345 | |
| Quiescent S2 | Kinase assay | 30 μM | completely abrogates TSA-induced hyperacetylation of H3K4me3 histones | 21518915 | |
| PC3 | Apoptosis assay | 20 μM | induces apoptosis | 21709130 | |
| Du145 | Apoptosis assay | 20 μM | induces apoptosis | 21709130 | |
| LNCaP | Apoptosis assay | 20 μM | induces apoptosis | 21709130 | |
| LAPC-4 | Apoptosis assay | 20 μM | induces apoptosis | 21709130 | |
| LNCaP | Function assay | 20 μM | decreases PSA secretion and p65 expression levels | 21709130 | |
| LAPC-4 | Function assay | 20 μM | decreases PSA secretion and p65 expression levels | 21709130 | |
| Kasumi-1 | Growth inhibitory assay | ~50 μM | inhibits cell proliferation | 23390536 | |
| SKNO-1 | Growth inhibitory assay | ~50 μM | inhibits cell proliferation | 23390536 | |
| Kasumi-1 | Kinase assay | ~10 μM | reduces expression of acetylated histone H3, c-kit and bcl-2 | 23390536 | |
| SKNO-1 | Kinase assay | ~10 μM | reduces expression of acetylated histone H3, c-kit and bcl-2 | 23390536 | |
| A549 | Function assay | 10 μM | enhances mitotic catastrophe | 24746574 | |
| NRK-52E | Function assay | 10 μM | inhibits Ang II-induced STAT3 nuclear translocation and the expression of TGF-β1, collagen IV and fibronectin | 25088002 | |
| PC12 | Growth inhibitory assay | ~12.5 μM | prevents TSA-induced neurite formation | 25128386 | |
| A549 | Function assay | ~50 μM | affects the viral life cycle and host response | 26711748 | |
| RAW264.7 | Function assay | ~30 μM | reduces pro-inflammatory gene expression | 26718586 | |
| MEMM | Kinase assay | 15 µM | decreases acetylation of histone H3 | 26921506 | |
| MEMM | Growth inhibitory assay | ~20 µM | inhibits cell proliferation | 26921506 | |
| MEMM | Apoptosis assay | 15 µM | induces the presence of the apoptosis protein, cleaved Caspase-3 | 26921506 | |
| T47D | Growth inhibitory assay | 10 μM | IC50=72 nM | 18381444 | |
| ZR-75-1 | Growth inhibitory assay | 10 μM | IC50=79 nM | 18381444 | |
| BT474 | Growth inhibitory assay | 10 μM | IC50=86 nM | 18381444 | |
| HCC1954 | Growth inhibitory assay | 10 μM | IC50=119 nM | 18381444 | |
| MDA-MB-453 | Growth inhibitory assay | 10 μM | IC50=975 nM | 18381444 | |
| MDA-MB-468 | Growth inhibitory assay | 10 μM | IC50=3208 nM | 18381444 | |
| SkBr3 | Growth inhibitory assay | 10 μM | IC50>10,000 nM | 18381444 | |
| MDA-MB-231 | Growth inhibitory assay | 10 μM | IC50>10,000 nM | 18381444 | |
| HCT116 | Growth inhibitory assay | 10 μM | IC50=5836 nM | 18381444 | |
| HT29 | Growth inhibitory assay | 10 μM | IC50>10,000 nM | 18381444 | |
| HFF | Growth inhibitory assay | 10 μM | IC50=7615 nM | 18381444 | |
| HN5 | Growth inhibitory assay | 10 μM | IC50>10,000 nM | 18381444 | |
| 786-0 | Growth inhibitory assay | 10 μM | IC50=4009 nM | 18381444 | |
| H157 | Growth inhibitory assay | 10 μM | IC50=2642 nM | 18381444 | |
| NCI-H460 | Growth inhibitory assay | 10 μM | IC50>2,500 nM | 18381444 | |
| SKOV-3 | Growth inhibitory assay | 10 μM | IC50=2126 nM | 18381444 | |
| OVCAR-3 | Growth inhibitory assay | 10 μM | IC50=2918 nM | 18381444 | |
| BXPC3 | Growth inhibitory assay | 10 μM | IC50=3141 nM | 18381444 | |
| MiaPaCa | Growth inhibitory assay | 10 μM | IC50=5433 nM | 18381444 | |
| PANC-1 | Growth inhibitory assay | 10 μM | IC50=8681 nM | 18381444 | |
| LNCaP | Growth inhibitory assay | 10 μM | IC50=147 nM | 18381444 | |
| DU145 | Growth inhibitory assay | 10 μM | IC50=3812 nM | 18381444 | |
| PC3 | Growth inhibitory assay | 10 μM | IC50>10,000 nM | 18381444 | |
| BT474 | Kinase assay | 10 μM | inhibits pGSK3β with IC50 of 160 nM | 18381444 | |
| 786-0 | Kinase assay | 10 μM | inhibits pGSK3β with IC50 of 150 nM | 18381444 | |
| LNCaP | Kinase assay | 10 μM | inhibits pGSK3β with IC50 of 43 nM | 18381444 | |
| PC3 | Kinase assay | 10 μM | inhibits pGSK3β with IC50 of 49 nM | 18381444 | |
| KARPAS-231 | Growth inhibitory assay | 10 μM | EC50=41 nM | 19064730 | |
| CCRFSB | Growth inhibitory assay | 10 μM | EC50=155 nM | 19064730 | |
| SUP B15 | Growth inhibitory assay | 10 μM | EC50=197 nM | 19064730 | |
| SD-1 | Growth inhibitory assay | 10 μM | EC50=320 nM | 19064730 | |
| RS4;11 | Growth inhibitory assay | 10 μM | EC50=654 nM | 19064730 | |
| MN-60 | Growth inhibitory assay | 10 μM | EC50=3602 nM | 19064730 | |
| Tanoue | Growth inhibitory assay | 10 μM | EC50=4517 nM | 19064730 | |
| RCH-ACV | Growth inhibitory assay | 10 μM | EC50=152 nM | 19064730 | |
| SEM | Growth inhibitory assay | 10 μM | EC50=202 nM | 19064730 | |
| KASUMI-2 | Growth inhibitory assay | 10 μM | EC50=225 nM | 19064730 | |
| REH | Growth inhibitory assay | 10 μM | EC50=288 nM | 19064730 | |
| 697 | Growth inhibitory assay | 10 μM | EC50=338 nM | 19064730 | |
| NALM-6 | Growth inhibitory assay | 10 μM | EC50=421 nM | 19064730 | |
| MHH-CALL–3 | Growth inhibitory assay | 10 μM | EC50=812 nM | 19064730 | |
| MHH-CALL–2 | Growth inhibitory assay | 10 μM | EC50=2114 nM | 19064730 | |
| J.GAMMA-1 | Growth inhibitory assay | 10 μM | EC50=65 nM | 19064730 | |
| JR45.01 | Growth inhibitory assay | 10 μM | EC50=68 nM | 19064730 | |
| A3 | Growth inhibitory assay | 10 μM | EC50=69 nM | 19064730 | |
| I 2.1 | Growth inhibitory assay | 10 μM | EC50=73 nM | 19064730 | |
| MOLT-3 | Growth inhibitory assay | 10 μM | EC50=74 nM | 19064730 | |
| P116 | Growth inhibitory assay | 10 μM | EC50=78 nM | 19064730 | |
| J.Cam1.6 | Growth inhibitory assay | 10 μM | EC50=79 nM | 19064730 | |
| I 9.2 | Growth inhibitory assay | 10 μM | EC50=80 nM | 19064730 | |
| LOUCY | Growth inhibitory assay | 10 μM | EC50=117 nM | 19064730 | |
| J.RT3-T3.5 | Growth inhibitory assay | 10 μM | EC50=123 nM | 19064730 | |
| 800000 | Growth inhibitory assay | 10 μM | EC50=163 nM | 19064730 | |
| Jurkat | Growth inhibitory assay | 10 μM | EC50=225 nM | 19064730 | |
| MOLT-4 | Growth inhibitory assay | 10 μM | EC50=232 nM | 19064730 | |
| Molt-16 | Growth inhibitory assay | 10 μM | EC50=241 nM | 19064730 | |
| CEM/C3 | Growth inhibitory assay | 10 μM | EC50=257 nM | 19064730 | |
| CEM/C2 | Growth inhibitory assay | 10 μM | EC50=271 nM | 19064730 | |
| CCRFCEM | Growth inhibitory assay | 10 μM | EC50=327 nM | 19064730 | |
| CEM/C1 | Growth inhibitory assay | 10 μM | EC50=382 nM | 19064730 | |
| SUPTI[VB] | Growth inhibitory assay | 10 μM | EC50=619 nM | 19064730 | |
| CCRF–HSB-2 | Growth inhibitory assay | 10 μM | EC50=2117 nM | 19064730 | |
| I 2.1 | Apoptosis assay | 10 μM | induces apoptosis | 19064730 | |
| I 9.2 | Apoptosis assay | 10 μM | induces apoptosis | 19064730 | |
| A3 | Apoptosis assay | 10 μM | induces apoptosis | 19064730 | |
| RD | Growth inhibitory assay | 10 μM | IC50>10 μM | 20740623 | |
| Rh41 | Growth inhibitory assay | 10 μM | IC50=33.8 nM | 20740623 | |
| Rh18 | Growth inhibitory assay | 10 μM | IC50=303 nM | 20740623 | |
| Rh30 | Growth inhibitory assay | 10 μM | IC50=4.81 μM | 20740623 | |
| BT-12 | Growth inhibitory assay | 10 μM | IC50>10 μM | 20740623 | |
| CHLA-266 | Growth inhibitory assay | 10 μM | IC50=1.22 μM | 20740623 | |
| TC-71 | Growth inhibitory assay | 10 μM | IC50=2.52 μM | 20740623 | |
| CHLA-9 | Growth inhibitory assay | 10 μM | IC50=591 nM | 20740623 | |
| CHLA-10 | Growth inhibitory assay | 10 μM | IC50=102 nM | 20740623 | |
| CHLA-258 | Growth inhibitory assay | 10 μM | IC50=1.05 μM | 20740623 | |
| GBM2 | Growth inhibitory assay | 10 μM | IC50=9.15 μM | 20740623 | |
| NB-1643 | Growth inhibitory assay | 10 μM | IC50=5.4 μM | 20740623 | |
| NB-Ebc1 | Growth inhibitory assay | 10 μM | IC50>10 μM | 20740623 | |
| CHLA-90 | Growth inhibitory assay | 10 μM | IC50>10 μM | 20740623 | |
| CHLA-136 | Growth inhibitory assay | 10 μM | IC50>10 μM | 20740623 | |
| NALM-6 | Growth inhibitory assay | 10 μM | IC50=265 nM | 20740623 | |
| COG-LL-317 | Growth inhibitory assay | 10 μM | IC50=6.49 nM | 20740623 | |
| RS4;11 | Growth inhibitory assay | 10 μM | IC50=147 nM | 20740623 | |
| MOLT-4 | Growth inhibitory assay | 10 μM | IC50=40 nM | 20740623 | |
| CCRF-CEM | Growth inhibitory assay | 10 μM | IC50=268 nM | 20740623 | |
| Kasumi-1 | Growth inhibitory assay | 10 μM | IC50=107 nM | 20740623 | |
| Karpas-299 | Growth inhibitory assay | 10 μM | IC50=2.93 μM | 20740623 | |
| Ramos-RA1 | Growth inhibitory assay | 10 μM | IC50=7.35 μM | 20740623 | |
| H1299 | Kinase assay | 10 μM | inhibits IKBKE-induced Akt Activation | 21908616 | |
| HPMCs | Function assay | reverses epithelial to mesenchymal transition of human peritoneal mesothelial cells | 26045780 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Tivantinib是第一个非ATP竞争性的c-Met抑制剂，在无细胞试验中Ki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。Tivantinib (ARQ 197) 可诱导G2/M期细胞阻滞和凋亡。 | ||
|---|---|---|---|
| 特性 | ARQ-197是第一个应用到晚期人类临床试验的c-Met选择性抑制剂。 | ||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | ARQ-197抑制HGF/c-met诱导的细胞反应。ARQ-197具有抗肿瘤活性，抑制A549, DBTRG和NCI-H441细胞增殖，IC50分别为0.38, 0.45, 0.29 μM。用ARQ-197处理，导致MAPK信号级联放大磷酸化降低，且阻断入侵和迁移。此外,没有内源性c-Met表达的NCI-H661细胞中c-Met异常表达，形成一种入侵表现型，也被ARQ-197抑制。加入浓度不断增加的ARQ-197不会明显影响ATP的Km值，但是用0.5 μM ARQ-197处理c-Met，则降低c-Met的Vmax值，降低3倍。ARQ-197降低Vmax而不影响ATP的Km值说明ARQ-197抑制c-Met是非ATP竞争抑制，也说明ARQ-197具有高度激酶选择性。ARQ-197抑制人类重组c-Met，具有恒定的Ki值，为355 nM。虽然使用过的ATP最高浓度为200 μM, 但是当ATP浓度为1 mM时，ARQ-197抑制c-Met效果不会降低。ARQ-197抑制c-Met磷酸化，且阻断下游c-Met信号通路。ARQ-197阻断组成型和配体调节的c-Met自磷酸化，通过增强c-Met活性, 反过来抑制下游c-Met效应器。ARQ-197作用于表达c-Met的人类癌细胞包括HT29, MKN-45, 和MDA-MB-231细胞，诱导caspase依赖的凋亡。[1] |
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|---|---|---|---|---|
| 激酶实验 | 体外c-Met SDS-PAGE 激酶试验 | |||
| 100 ng重组c-Met蛋白和浓度不断增高ARQ-197在室温下预温育30分钟。随后，100 μM 聚Glu-Tyr底物和含5 μCi[γ-32P]ATP的不同浓度ATP加到反应混合物中。反应在室温下进行5分钟，然后加入5 μL SDS-聚丙烯酰胺胶,降低样本缓冲液。上样到7.5%丙烯酰胺胶上，进行SDS-PAGE。通过放射自显影观察到磷酸化的聚Glu-Tyr底物。通过光密度法测定c-Met活性。 | ||||
| 细胞实验 | 细胞系 | T29, MKN-45和MDA-MB-231细胞 | ||
| 浓度 | 0.03-10 μM | |||
| 孵育时间 | 24, 32,和48细胞 | |||
| 方法 | HT29,MKN-45,和MDA-MB-231细胞按每孔5×103个接种在96孔板上，孔中有含10% FBS的培养基，在黑暗中过夜处理。第二天,用浓度不断增长的ARQ-197 (0.03-10 μM)在37oC下处理细胞24,32,和48 小时。ARQ-197处理后，移除培养基，细胞在含2 μg/mL Hoescht 33342的标签溶液(10 mM HEPES, 140 mM NaCl,和6 mM CaCl2)中温育至少10分钟, 用Annexin V-FITC(稀释500倍)和1 μg/mL碘化丙锭染色。进行高含量的图像采集和分析，每孔获取四个图像。 4,6-二脒基-2-苯基吲哚, FITC, 和罗丹明通道分别在16.7 ms/10%, 500 ms/35% ,和300 ms/30% 进行处理。处理图像，测定每组通道和每种情况下的阳性细胞数。此外,在有或者没有25,50,和100 μM ZvAD-FMK存在条件下，HT29细胞用浓度不断增加的ARQ-197处理32小时。所有实验重复进行三次。测定抑制c-Met是否导致细胞凋亡，当使用siRNA分解磷酸甘油醛脱氢酶(GAPDH)和c-Met时ARQ-197的作用效果。HT29, MKN-45,和MDA-MB-231细胞转染无靶点对照 siRNA, GAPDH靶点对照siRNA, 或met靶点siRNA。3天后，使用特点抗体测定c-Met, GAPDH, 和 β-actin表达水平。为了测定caspase依赖是否影响，HT29, MKN-45, 和MDA-MB-231细胞转染 met靶点 siRNA，进行2天。然后在有或没有浓度不断增高的ZvAD-FMK存在下再温育1天。无靶点siRNA和GAPDH siRNA也转染，作为对照。然后用Annexin V-FITC和碘化丙锭进行细胞染色,测定凋亡细胞百分数。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | cMET / p-cMET / p-AKT / p-ERK / p-rpS6 |
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23022995 | |
| Growth inhibition assay | Cell viability |
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23598276 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | ARQ-197处理 HT29,MKN-45,和MDA-MB-231三种移植瘤模型，肿瘤生长率分别降低66%,45%,和79%。ARQ-197按200 mg/kg剂量口服给药这三种移植瘤模型，显示体重都没有明显改变。药效学方面，ARQ-197作用于人类结肠移植瘤HT29，强抑制c-Met的磷酸化, ARQ-197按200 mg/kg剂量单独口服给药24小时后，c-Met自磷酸化强烈下降。总之，ARQ-197抑制人类c-Met依赖的移植瘤生长。[1] |
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|---|---|---|
| 动物实验 | Animal Models | 携带HT29,MKN-45,或MDA-MB-231移植瘤的无胸腺裸鼠 |
| Dosages | 200 mg/kg | |
| Administration | 口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02150733 | Completed | Hepatic Impairment|Solid Tumor|Cancer |
Daiichi Sankyo|Medpace Inc. |
April 2014 | Phase 1 |
| NCT01892527 | Completed | Colorectal Cancer Metastatic|C-met Overexpression |
Armando Santoro MD|Istituto Clinico Humanitas |
March 2013 | Phase 2 |
| NCT02049060 | Completed | Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of Lung |
Armando Santoro MD|Istituto Clinico Humanitas |
January 2013 | Phase 1|Phase 2 |
| NCT01755767 | Completed | Hepatocellular Carcinoma |
Daiichi Sankyo|ArQule Inc. a subsidiary of Merck Sharp & Dohme LLC a subsidiary of Merck & Co. Inc. (Rahway NJ USA) |
December 27 2012 | Phase 3 |
化学信息&溶解度
| 分子量 | 369.42 | 分子式 | C23H19N3O2 |
| CAS号 | 905854-02-6 | SDF | Download Tivantinib SDF |
| Smiles | C1CC2=C3C(=CC=C2)C(=CN3C1)C4C(C(=O)NC4=O)C5=CNC6=CC=CC=C65 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 73 mg/mL ( (197.6 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 35 mg/mL (94.74 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
Are there any other solutions (apart from DMSO) I can dissolve S2753 for in vivo experiment?
回答：
S2753 Tivantinib (ARQ 197) can be dissolved in 1% methylcellulose at15 mg/ml as a suspension.
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