AST 487
- CAS No.
- 630124-46-8
- Chemical Name:
- AST 487
- Synonyms
- CS-562;AST 487;NVP-AST 487;AST487 (NVP- AST487);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;3-{4-[(4-ETHYLPIPERAZIN-1-YL)METHYL]-3-(TRIFLUOROMETHYL)PHENYL}-1-(4-{[6-(METHYLAMINO)PYRIMIDIN-4-YL]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]-
- CBNumber:
- CB02627342
- Molecular Formula:
- C26H30F3N7O2
- Molecular Weight:
- 529.56
- MDL Number:
- MFCD11983171
- MOL File:
- 630124-46-8.mol
- MSDS File:
- SDS
| Melting point | 162-164°C |
|---|---|
| Boiling point | 563.1±50.0 °C(Predicted) |
| Density | 1.341±0.06 g/cm3(Predicted) |
| storage temp. | under inert gas (nitrogen or Argon) at 2-8°C |
| solubility | DMSO (Slightly), Methanol (Slightly) |
| pka | 13.33±0.70(Predicted) |
| form | Solid |
| color | White to Light Yellow |
| FDA UNII | W34UO2M4T6 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
AST 487 price More Price(25)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML2363 | AST487 ≥98% (HPLC) | 630124-46-8 | 5MG | $99 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML2363 | AST487 ≥98% (HPLC) | 630124-46-8 | 25MG | $399 | 2024-03-01 | Buy |
| Cayman Chemical | 19477 | AST-487 ≥98% | 630124-46-8 | 1mg | $33 | 2024-03-01 | Buy |
| Cayman Chemical | 19477 | AST-487 ≥98% | 630124-46-8 | 5mg | $112 | 2024-03-01 | Buy |
| Cayman Chemical | 19477 | AST-487 ≥98% | 630124-46-8 | 10mg | $208 | 2024-03-01 | Buy |
AST 487 Chemical Properties,Uses,Production
Uses
N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N''-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea is an inhibitor of RET, FLT3, KDR, c-Abl and c-Kit. Also, it prevent the growth of human thyroid cancer cells. It is a COVID19-related research product.
Uses
AST-487 is an inhibitor of RET (IC50 = 0.88 μM), FLT3 (Ki = 0.52 μM), KDR (IC50 = 0.17 μM), c-Abl (IC50 = 0.02 μM), and c-Kit (IC50 = 0.5 μM). It has been shown to inhibit RET autophosphorylation and activation of downstream effectors and to prevent the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. In xenografts of NIH3T3 cells expressing oncogenic RET and of the MTC cell line TT in nude mice, AST-487 dose dependently inhibited tumor growth. It also demonstrates antiproliferative effects on primary cells from acute myelocytic leukemia patients and on cell lines expressing FLT3-ITD or FLT3 kinase domain point mutants.[Cayman Chemical]
Biological Activity
ast487 is an inhibitor of ret kinase with ic50 value of 0.88μm [1].ast487 belongs to the n,n’-diphenyl urea class. it inhibit the activity of ret kinase as well as many other kinases( such as kdr, flt-3 and c-kit) in vitro. in the cell assay, the inhibition effect of ast487 is displayed both in pc-ret/ptc3 cells and tt cells, which harbor an endogenous activating point mutation of ret (retc634w). ast487 decreases ret autophosphorylation and activation of plcγ and erk with a dose-dependent manner. additionally, ast487 is also found to inhibit the growth of human thyroid cancer cell lines with ret, but not braf mutations. it supports the selectivity of ast487 for ret. in vivo assay shows that ast487 causes significant reductions in the size of nih3t3-retc634w xenografts with doses >30 mg/kg/d and oral administration of ast487 at 50 or 30 mg/kg/d decreases mean tumor volume in mice [1].
target
RET kinase
References
[1] nagako akeno-stuart, michelle croyle, jeffrey a. knauf, et al. the ret kinase inhibitor nvp-ast487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. cancer res. 2007, 67:6956-6964.
AST 487 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7553 | 61 |
| MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4863 | 58 |
| AdooQ BioScience, LLC | +1 (866) 930-6790 | info@adooq.com | United States | 2784 | 58 |
