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Chemical Structure : NVP-AST487
CAS No.: 630124-46-8
Catalog No.: PC-61590Not For Human Use, Lab Use Only.
NVP-AST487 (AST487) is a potent, oral bioavailable RET kinase inhibitor with IC50 of 0.88 uM, also inhibits KDR, Flt-4, Flt-3, c-Kit and c-Abl in vitro (IC50=0.1-1.2 uM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $188 | In stock | |
| 25 mg | $388 | In stock | |
| 100 mg | $898 | In stock | |
| 500 mg | Get quote | ||
| 1 g | Get quote |
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NVP-AST487 (AST487) is a potent, oral bioavailable RET kinase inhibitor with IC50 of 0.88 uM, also inhibits KDR, Flt-4, Flt-3, c-Kit and c-Abl in vitro (IC50=0.1-1.2 uM).
NVP-AST487 displays little to no activity against EGFR, HER2, PDK1 and PKB (IC50>5 uM).
NVP-AST487 inhibits RET autophosphorylation and activation of PLCγ and ERK, inhibits the growth of thyroid cancer cell lines with activating mutations of RET (RET C634W, IC50= 5 nM).
NVP-AST487 inhibits the growth of NIH3T3-RETC634W xenografts in mice.
AST487 also potently inhibits CDKL5 activity with IC50 of 87 nM.
| M.Wt | 529.56 | |
| Formula | C26H30F3N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(4-((6-(methylamino)pyrimidin-4-yl)oxy)phenyl)urea |
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1. Akeno-Stuart N, et al. Cancer Res. 2007 Jul 15;67(14):6956-64.
2. Weisberg E, et al. Blood. 2008 Dec 15;112(13):5161-70.
3. Andreucci E, et al. Oncotarget. 2016 Dec 6;7(49):80543-80553.
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