PLX-4720
PLX-4720是一种有效的，选择性的B-RafV600E抑制剂，无细胞试验中IC50为13 nM，同样有效地作用于c-Raf-1(Y340D和Y341D突变型)，作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。
PLX-4720 Chemical Structure
CAS: 918505-84-7
产品质控
批次：
纯度：
99.98%
99.98
常与PLX-4720一起在实验中被使用的化合物
PLX-4720和Dactolisib治疗可降低Colo-205异种移植物中的pERK和pAKT水平。
Schulte ML, et al. Mol Imaging Biol. 2017 Jun;19(3):421-428.
PLX-4720和Navitoclax可以增强BRAF抑制剂的临床疗效。
Frederick DT, et al. Cancer Res (2013) 73 (8_Supplement): 1724.
PLX-4720和Dabrafenib可显着减少BRAF突变黑色素瘤细胞因脑脊液存在而死亡。
Seifert H, et al. Pigment Cell Melanoma Res. 2016 Jan;29(1):92-100.
PLX-4720和NMS-E973在A375黑色素瘤细胞中显示出协同抗增殖活性。
Fogliatto G, et al. Clin Cancer Res. 2013 Jul 1;19(13):3520-32.
PLX-4720和SB431542共处理消除了低剂量PLX-4720在Colo829和A375(M2)细胞中引起的细胞生长增加。
Spender LC, et al. Oncotarget. 2016 Dec 13; 7(50): 81995–82012.
PLX-4720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 |
|---|---|---|---|---|---|
| A375 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.5 μM. | 29461827 | |
| SK-LU-1 | Growth Inhibition Assay | IC50=12.2655 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=11.7178 μM | SANGER | ||
| SK-HEP-1 | Growth Inhibition Assay | IC50=11.3527 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=11.2404 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=10.8472 μM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=10.8274 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=10.458 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=10.4212 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=10.0149 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=9.6048 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=9.56999 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=9.05178 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=8.75314 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=8.41516 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=8.07068 μM | SANGER | ||
| COLO-741 | Growth Inhibition Assay | IC50=8.01679 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=7.36907 μM | SANGER | ||
| BCPAP | Growth Inhibition Assay | IC50=7.21764 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=6.81931 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=6.45423 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=6.22493 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=6.21373 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=6.18129 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=6.14924 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=6.10946 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=6.00902 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=5.97603 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=5.80283 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=5.1873 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=4.73908 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=4.72164 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=4.53325 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=4.49179 μM | SANGER | ||
| CP66-MEL | Growth Inhibition Assay | IC50=4.15927 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=3.55266 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=3.40176 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=2.92232 μM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=2.87946 μM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=2.72673 μM | SANGER | ||
| KP-4 | Growth Inhibition Assay | IC50=2.30787 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=2.11969 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.04978 μM | SANGER | ||
| HTC-C3 | Growth Inhibition Assay | IC50=1.66294 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=1.6086 μM | SANGER | ||
| SK-MEL-30 | Growth Inhibition Assay | IC50=1.33386 μM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=1.14963 μM | SANGER | ||
| COLO-679 | Growth Inhibition Assay | IC50=1.10464 μM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=1.04569 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=0.88692 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=0.87844 μM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=0.86796 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.79644 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=0.76148 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=0.70702 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=0.68614 μM | SANGER | ||
| A375 | Growth Inhibition Assay | IC50=0.67359 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=0.51568 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=0.41422 μM | SANGER | ||
| MEL-HO | Growth Inhibition Assay | IC50=0.41179 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=0.38968 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=0.38477 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=0.36329 μM | SANGER | ||
| G-361 | Growth Inhibition Assay | IC50=0.34637 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=0.32589 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=0.29784 μM | SANGER | ||
| M14 | Growth Inhibition Assay | IC50=0.21757 μM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=0.15131 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.14166 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=0.07457 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=12.3932 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=12.6062 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=12.7169 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=12.8833 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=13.9576 μM | SANGER | ||
| KYSE-140 | Growth Inhibition Assay | IC50=14.0753 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=14.3359 μM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=14.8492 μM | SANGER | ||
| D-542MG | Growth Inhibition Assay | IC50=14.9222 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=14.9932 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=15.2684 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=15.4293 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=15.4305 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=15.4458 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=15.7616 μM | SANGER | ||
| SCH | Growth Inhibition Assay | IC50=15.7835 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=16.0646 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=16.4862 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=16.8107 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=17.118 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=17.3071 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=17.4965 μM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=17.7248 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=17.818 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=18.3172 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=18.5708 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=19.5711 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=19.5858 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=19.7642 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=19.9887 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=20.0478 μM | SANGER | ||
| NCI-H1755 | Growth Inhibition Assay | IC50=20.4764 μM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=20.5748 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=20.6756 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=20.7056 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=20.7201 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=21.1915 μM | SANGER | ||
| IGR-1 | Growth Inhibition Assay | IC50=21.3796 μM | SANGER | ||
| HOP-92 | Growth Inhibition Assay | IC50=21.4987 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=21.7381 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=21.8624 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=22.1203 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=22.244 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=22.5155 μM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=22.6059 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=22.6751 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=22.7366 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=22.7979 μM | SANGER | ||
| HT-1197 | Growth Inhibition Assay | IC50=23.0817 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=23.6412 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=24.7595 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=24.8744 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=25.0023 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=25.2751 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=25.3192 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=25.938 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=27.2018 μM | SANGER | ||
| COR-L23 | Growth Inhibition Assay | IC50=27.2813 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=27.368 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=27.6706 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=27.944 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=28.1604 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=28.2814 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=28.713 μM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=28.8845 μM | SANGER | ||
| TCCSUP | Growth Inhibition Assay | IC50=28.9272 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=29.5682 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=32.1964 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=32.3301 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=32.5973 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=33.1648 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=33.6504 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=33.7236 μM | SANGER | ||
| ACHN | Growth Inhibition Assay | IC50=33.8385 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=33.8544 μM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=33.8971 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=35.7292 μM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=35.8132 μM | SANGER | ||
| HMV-II | Growth Inhibition Assay | IC50=36.0774 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=37.6455 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=38.0015 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=38.1026 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=38.1332 μM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=38.1615 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=38.79 μM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=39.8629 μM | SANGER | ||
| KP-N-YN | Growth Inhibition Assay | IC50=40.4285 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=40.4957 μM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=43.274 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=43.2895 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=43.3071 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=44.9959 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=45.65 μM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=46.0359 μM | SANGER | ||
| NY | Growth Inhibition Assay | IC50=46.1778 μM | SANGER | ||
| EFM-19 | Growth Inhibition Assay | IC50=46.7533 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=46.7806 μM | SANGER | ||
| UM-UC-3 | Growth Inhibition Assay | IC50=46.8059 μM | SANGER | ||
| HT-29 | Growth Inhibition Assay | IC50=47.8792 μM | SANGER | ||
| LN-405 | Growth Inhibition Assay | IC50=48.0827 μM | SANGER | ||
| NCI-H727 | Growth Inhibition Assay | IC50=48.7726 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=48.9676 μM | SANGER | ||
| GMS-10 | Growth Inhibition Assay | IC50=49.2974 μM | SANGER | ||
| MEL-JUSO | Growth Inhibition Assay | IC50=49.347 μM | SANGER | ||
| insect cells | Function assay | Inhibition of N-terminal His-tagged BRAF V600E mutant (unknown origin) expressed in baculovirus infected insect cells co-expressing CDC37 using biotinylated-MEK as substrate by AlphaScreen assay, IC50 = 0.013 μM. | 29461827 | ||
| A375 | Function assay | Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by AlphaScreen assay, IC50 = 0.044 μM. | 29461827 | ||
| A375 | Function assay | Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK, IC50 = 0.046 μM. | 22808911 | ||
| A375 | Antiproliferative assay | Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras, IC50 = 0.5 μM. | 22808911 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant, IC50 = 27 μM. | 22808911 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | PLX-4720是一种有效的，选择性的B-RafV600E抑制剂，无细胞试验中IC50为13 nM，同样有效地作用于c-Raf-1(Y340D和Y341D突变型)，作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | PLX-4720高亲和力与活性B-RafV600E和c-Raf-1Y340D/Y341D结合，作用于野生型B-Raf选择性>10倍,作用于其他激酶如Frk, Src, Fak, FGFR, 和Aurora A 选择性>100倍，IC50为1.3-3.4 μM。与有效的选择性相一致, PLX-4720作用于携带B-RafV600E的细胞系，显著抑制ERK磷酸化，IC50为14-46 nM, 但是对携带野生型B-Raf的细胞没有作用效果。PLX-4720 作用于携带B-RafV600E致癌基因（如COLO205, A375, WM2664, 和 COLO829）的肿瘤细胞系，显著抑制细胞生长，GI50 分别为 0.31 μM, 0.50 μM, 1.5 μM, 和 1.7 μM。此外, 1 μM PLX-4720 只有作用于B-RafV600E-阳性1205Lu细胞, 诱导细胞周期停滞和凋亡，而作用于B-Raf 野生型C8161细胞则无此效果。[1]10 μM PLX-4720 处理PTEN+细胞，诱导BIM表达，比PTEN-细胞系(4倍-fold)高14倍，说明PTEN-细胞系抗PLX-4720诱导的凋亡。[2] | |||
|---|---|---|---|---|
| 激酶实验 | 体外Raf激酶活性实验 | |||
| 通过测量生物素-MEK蛋白，使用Perkin-Elmer's AlphaScreen 技术测定体外野生型和突变型Raf的激酶活性。在20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% Tween-20, 100 nM 生物素-MEK 蛋白,多种ATP浓度,及浓度不断增高的PLX-4720混合物中在室温下进行每组酶(0.1 ng)反应，反应体积为20-μL。 在 2, 5, 8, 10, 20,和 30分钟加入5 μL含20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, 和 0.3% BSA的溶液终止反应。终止液包括磷酸-MEK抗体, 链霉亲和素包被的供体珠，和AlphaScreen蛋白 A检测试剂盒中的蛋白A受体珠。抗体和小株在终止液中在室温下黑暗温育30分钟。抗体最终按 1:2,000稀释,每个小珠终浓度为 10 μg/mL。实验板在室温下温育1小时，然后在 PerkinElmer AlphaQuest 读数器上读数。 | ||||
| 细胞实验 | 细胞系 | COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, 和C8161 | ||
| 浓度 | 溶于DMSO, 终浓度为~1 mM | |||
| 孵育时间 | 24, 48, 和 72小时 | |||
| 方法 | 使用不同浓度PLX-4720 for处理细胞 24, 48,和72小时通过 CellTiter-GLO荧光细胞活性检测或MTT实验测定细胞增殖。为了分析细胞周期, 收集上清液和细胞, 制成颗粒，与70%乙醇混合。在使用碘化丙啶 (10 μg/mL)染色前,细胞在0.5 mg/mL RNase I 中37oC下温育1小时，除去残留RNA污染样本。使用EPICS XL仪分析样本。为了测定凋亡, 获得培养基和细胞，制成颗粒，然后使用膜联蛋白-FITC和碘化丙啶染色。然后再使用EPICS XL仪分析样本。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | pAkt(Ser473) / pAkt(Thr308) p27 / Cyclin D1 / pRb p-EGFR 1173 / EGFR / p-Akt / Akt p-MEK / MEK / p-ERK / ERK / p-FAK(S910) |
|
21828154 | |
| Immunofluorescence | ZKSCAN3 / TFEB LAMP1 |
|
30979895 | |
| Growth inhibition assay | Cell viability |
|
27848137 | |
| ELISA | mIFN-γ |
|
23204132 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | PLX-4720每天按20 mg/kg剂量口服给药依赖B-RafV600E的COLO205移植瘤，显著延迟肿瘤生长，且引起肿瘤衰退, 即使按1 g/kg剂量处理也不会对小鼠造成明显的不利影响。PLX-4720按 100 mg/kg剂量处理 携带B-RafV600E的1205Lu 移植瘤，每天两次，几乎完全消除肿瘤, 而对携带野生型B-Raf的C8161 移植瘤则没有作用活性。PLX-4720 作用于含V600E突变细胞的抗癌效果与阻断MAPK通路相关。[1] PLX-4720每天按30 mg/kg剂量处理8505c肿瘤，显著抑制肿瘤生长，抑制达90%以上,也显著降低远处肺转移。[3] | |
|---|---|---|
| 动物实验 | Animal Models | 皮下移植 COLO205 细胞的雌性无胸腺NCr nu/nu小鼠, 携带1205Lu或C8161 细胞的SCID小鼠 |
| Dosages | 5, 20, 或100 mg/kg | |
| Administration | 口服饲喂，每天一次或两次 | |
化学信息&溶解度
| 分子量 | 413.83 | 分子式 | C17H14ClF2N3O3S |
| CAS号 | 918505-84-7 | SDF | Download PLX-4720 SDF |
| Smiles | CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)Cl)F | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 83 mg/mL ( (200.56 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
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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* 必填项
常见问题及建议解决方法
问题 1:
What would you recommend to make working solution for intraperitoneal injection into mice?
回答：
PLX4720 has very limited solubility in aqueous solution and for this reason, we recommend oral gavage to administer this compound as not fully dissolved suspension can be used in oral gavage feeding.
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