RET激酶抑制剂(AST 487)
AST 487
CAS: 630124-46-8
Molecular Formula: C26H30F3N7O2
RET激酶抑制剂(AST 487) - Names and Identifiers
| Name | AST 487 |
| Synonyms | CS-562 AST 487 NVP-AST 487 3-{4-[(4-ETHYLPIPERAZIN-1-YL)METHYL]-3-(TRIFLUOROMETHYL)PHENYL}-1-(4-{[6-(METHYLAMINO)PYRIMIDIN-4-YL]OXY}PHENYL)UREA 1-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(4-((6-(methylamino)pyrimidin-4-yl)oxy)phenyl)urea 1-{4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl}-3-(4-{[6-(methylamino)-4-pyrimidinyl]oxy}phenyl)urea N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N'-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea N-[4-[(4-ETHYL-1-PIPERAZINYL)METHYL]-3-(TRIFLUOROMETHYL)PHENYL]-N'-[4-[[6-(METHYLAMINO)-4-PYRIMIDINYL]OXY]PHENYL]UREA Urea,N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N'-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]- |
| CAS | 630124-46-8 |
| EINECS | 205-525-8 |
RET激酶抑制剂(AST 487) - Physico-chemical Properties
| Molecular Formula | C26H30F3N7O2 |
| Molar Mass | 529.56 |
| Density | 1.341±0.06 g/cm3(Predicted) |
| Melting Point | 162-164°C |
| Boling Point | 563.1±50.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Light Yellow |
| pKa | 13.33±0.70(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
| In vitro study | A number of other kinases are also similarly inhibited by AST 487 (NVP-AST487) in the in vitro kinase assays, including KDR (IC 50 =170 nM), Flt-4 (IC 50 =790 nM), Flt-3 (IC 50 =520 nM), c-Kit (IC 50 =500 nM), and c-Abl (IC 50 =20 nM). AST 487 potently inhibits the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. Both GDNF/GFRα1 and persephin-induced calcitonin mRNA are markedly inhibited by coincubation with 100 nM of AST 487 in MTC-M cells. AST 487 is a novel, mutant FLT3 inhibitor. AST 487 is tested in biochemical assays for inhibition of Flt-3 kinase activity. The K i is determined to be 0.12 μM. Besides Flt-3, NVP-AST487 inhibits RET, KDR, c-Kit, and c-Abl kinase with IC 50 values below 1 μM. Treatment of FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells with AST 487 potently inhibits cellular proliferation (IC 50 <5 nM). AST 487 treatment of FLT3-ITD-Ba/F3 cells with 0.01 μM AST 487 results in complete cell killing compare with approximately 50% killing of AML patient samples at the same concentration. |
| In vivo study | After a single oral administration of 15 mg/kg of AST 487 to OF1 mice, a mean peak plasma level (C max ) of 0.505±0.078 μM SE is achieved after 0.5 h. Similar levels of AST 487 are found in the plasma of mice up to 6 h after oral administration, with a C last of 21±4 nM at 24 h. The oral bioavailability is calculated to be 9.7% with a t 1/2 terminal elimination of 1.5 h. |
RET激酶抑制剂(AST 487) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.888 ml | 9.442 ml | 18.884 ml |
| 5 mM | 0.378 ml | 1.888 ml | 3.777 ml |
| 10 mM | 0.189 ml | 0.944 ml | 1.888 ml |
| 5 mM | 0.038 ml | 0.189 ml | 0.378 ml |
Last Update：2024-01-02 23:10:35
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