c-RET
シグナル伝達経路
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 |
| S8189 | BAW2881 (NVP-BAW2881) | <1 mg/mL | 84 mg/mL | 20 mg/mL |
| S8348 | BMS-935177 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S5077 | Regorafenib Monohydrate | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S8696 | 2-D08 | <1 mg/mL | 54 mg/mL | <1 mg/mL |
| S8518 | AD80 | <1 mg/mL | 94 mg/mL | 94 mg/mL |
- c-RET阻害剤(8)
- 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) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. |
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
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| S1107 |
Danusertib (PHA-739358)Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2. |
c, Upper panel: viable cell number of FLT3-ITD-positive AML patient samples incubated with vandetanib, danusertib, or DMSO for 7 days in methylcellulose. The mean ± SD of duplicates is shown. Lower panel: viability and proliferation of mutant FLT3-positive AML cell lines and one AML patient sample treated with vandetanib and crenolanib alone or in combination for 3 days. The calculated additive effects of both inhibitors according to the Bliss Independence model are indicated by the dashed lines. The mean ± SD of four (cell lines) or two (patient sample) independent experiments is shown. P-values were calculated using one-way ANOVA followed by Dunnett’s test for multiple comparisons. *P ≤ 0.05; **P ≤ 0.01; ***P ≤ 0.001.
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| S2692 |
TG101209TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations. |
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.
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| S8189 |
BAW2881 (NVP-BAW2881)BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET at 45-72 nM concentrations. |
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| S8348新 |
BMS-935177 |
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| S5077新 |
Regorafenib Monohydrate |
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| S8696新 |
2-D08 |
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| S8518新 |
AD80AD80, a multikinase inhibitor, shows strong activity against human RET, BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM. |
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