c-RET
信号経路図
研究分野
- 阻害剤の選択性比較
- 溶解度
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1178 | Regorafenib (BAY 73-4506) | <1 mg/mL | 97 mg/mL | <1 mg/mL |
| S1107 | Danusertib (PHA-739358) | <1 mg/mL | 95 mg/mL | <1 mg/mL |
| S2692 | TG101209 | <1 mg/mL | 102 mg/mL | <1 mg/mL |
| S8518 | AD80 | <1 mg/mL | 94 mg/mL | 94 mg/mL |
- c-RET阻害剤(4)
- 新c-RET製品
| 製品コード | 製品説明 | 文献中の使用例 | お客様のフィードバック |
|---|---|---|---|
| S1178 |
Regorafenib (BAY 73-4506)Regorafenib (BAY 73-4506)は一種の多ターゲット阻害剤で、無細胞試験でVEGFR1、VEGFR2、VEGFR3、PDGFR-β、Kit、RETとRaf-1に作用する時のIC50値が13 nM、4.2 nM、46 nM、22 nM、7 nM、1.5 nMと2.5 nMにそれぞれ分かれることです。 |
Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05
|
|
| S1107 |
Danusertib (PHA-739358)Danusertib (PHA-739358)は一種のオーロラキナーゼ阻害剤です。Danusertib (PHA-739358)はオーロラA/B/Cに作用して、無細胞試験でIC50値が13 nM/79 nM/61 nMになリますが、Abl、TrkA、c-RETとFGFR1に適度に作用します。Danusertib (PHA-739358)はLck、VEGFR2/3、c-KitとCDK2等に作用する効果が少し弱いです。臨床2期。 |
Mice bearing subcutaneous allografts of conditional patched mutant tumor cells were treated twice weekly with vehicle (saline) or 30 mg/kg PHA-739358. (B)Images of tumors. (C) Tumor weights. Each point represents a single tumor, and grey lines represent mean tumor weights, which were significantly different between vehicle and PHA-739358 treated mice (p < 0.05, based on paired two-tailed t-test).
|
|
| S2692 |
TG101209TG101209は一種の選択性JAK2阻害剤で、無細胞試験でIC50値が6 nMになって、Flt3とRETに作用する効果が少し弱くて、なお IC50値が25 nMと17 nMに分かれて、JAK2に作用する選択性はJAK3に作用する選択性より30倍程度が高くなって、JAK2V617FとMPLW515L/K突然変異体に敏感です。 |
Primary plasma cells from MM patient 5 used were incubated with indicated concentrations of LCL161, TG101209 or the combination for 24 h. Western blot analysis were performed to examine expression levels of pStat3 and IAPs.
|
|
| S8518新 |
AD80 |
-Erlotinib-Carboplatin-Gemcitabine-Doxorubicin(Adriamycin)-Proc-Natl-Acad-Sci-USA-20150730.gif)
| 製品コード | 製品説明 | 文献中の使用例 | お客様のフィードバック |
|---|---|---|---|
| S1178 |
Regorafenib (BAY 73-4506)Regorafenib (BAY 73-4506)は一種の多ターゲット阻害剤で、無細胞試験でVEGFR1、VEGFR2、VEGFR3、PDGFR-β、Kit、RETとRaf-1に作用する時のIC50値が13 nM、4.2 nM、46 nM、22 nM、7 nM、1.5 nMと2.5 nMにそれぞれ分かれることです。 |
Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05
|
|
| S1107 |
Danusertib (PHA-739358)Danusertib (PHA-739358)は一種のオーロラキナーゼ阻害剤です。Danusertib (PHA-739358)はオーロラA/B/Cに作用して、無細胞試験でIC50値が13 nM/79 nM/61 nMになリますが、Abl、TrkA、c-RETとFGFR1に適度に作用します。Danusertib (PHA-739358)はLck、VEGFR2/3、c-KitとCDK2等に作用する効果が少し弱いです。臨床2期。 |
Mice bearing subcutaneous allografts of conditional patched mutant tumor cells were treated twice weekly with vehicle (saline) or 30 mg/kg PHA-739358. (B)Images of tumors. (C) Tumor weights. Each point represents a single tumor, and grey lines represent mean tumor weights, which were significantly different between vehicle and PHA-739358 treated mice (p < 0.05, based on paired two-tailed t-test).
|
|
| S2692 |
TG101209TG101209は一種の選択性JAK2阻害剤で、無細胞試験でIC50値が6 nMになって、Flt3とRETに作用する効果が少し弱くて、なお IC50値が25 nMと17 nMに分かれて、JAK2に作用する選択性はJAK3に作用する選択性より30倍程度が高くなって、JAK2V617FとMPLW515L/K突然変異体に敏感です。 |
Primary plasma cells from MM patient 5 used were incubated with indicated concentrations of LCL161, TG101209 or the combination for 24 h. Western blot analysis were performed to examine expression levels of pStat3 and IAPs.
|
|
| S8518新 |
AD80 |
