- 抑制剂
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- 生物试剂
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白实验
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag亲和凝胶
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 细胞核与细胞浆蛋白抽提试剂盒
- 免疫磁珠
- 蛋白酶抑制剂Cocktail
- 蛋白酶抑制剂Cocktail(DMSO储液)
- 磷酸酶抑制剂Cocktail
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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(PMID) |
|---|---|---|---|---|---|
| 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 |
|
| 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 | p-MEK / MEK / p-ERK / ERK / p-FAK(S910) p-EGFR 1173 / EGFR / p-Akt / Akt p27 / Cyclin D1 / pRb pAkt(Ser473) / pAkt(Thr308) |
|
23076151 | |
| Immunofluorescence | LAMP1 ZKSCAN3 / TFEB |
|
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) | |||
|
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 |
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体内溶解配方 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：
Due to its very limited solubility in aqueous solution, this compound can be administered as a not fully dissolved suspension via oral gavage. For this reason, we recommend oral gavage for its administration.
