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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A413573-2mg | 2mg | In stock | $42.90 | |
A413573-5mg | 5mg | In stock | $88.90 | |
A413573-10mg | 10mg | In stock | $147.90 | |
A413573-25mg | 25mg | In stock | $246.90 | |
A413573-50mg | 50mg | In stock | $444.90 | |
A413573-100mg | 100mg | In stock | $840.90 |
Abl Selective Inhibitors
Synonyms | NVP-AST487 | NVP-AST-487 | AC-5620 | W34UO2M4T6 | HY-15002 | ZB1589 | BDBM31085 | 1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea | DTXSID70212239 | Q27074554 | HY-W009498 | 1-[4-[(4-eth |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Tyrosine-protein kinase receptor RET inhibitor |
Product Description | Information AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor ofFlt3with ki of 0.12 μM.Besides FLT3, AST487 also inhibitsRET,KDR,c-KIT,and c-ABL kinasewith IC50 values below 1 μM. Targets RET ; KDR ; c-Kit ; c-Abl ; FLT3 (Cell-free assay) ; ;; 0.12 μM(Ki) |
ALogP | 3.8 |
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IUPAC Name | 1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea |
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INCHI | InChI=1S/C26H30F3N7O2/c1-3-35-10-12-36(13-11-35)16-18-4-5-20(14-22(18)26(27,28)29)34-25(37)33-19-6-8-21(9-7-19)38-24-15-23(30-2)31-17-32-24/h4-9,14-15,17H,3,10-13,16H2,1-2H3,(H,30,31,32)(H2,33,34,37) |
InChi Key | ODPGGGTTYSGTGO-UHFFFAOYSA-N |
Canonical SMILES | CCN1CCN(CC1)CC2=C(C=C(C=C2)NC(=O)NC3=CC=C(C=C3)OC4=NC=NC(=C4)NC)C(F)(F)F |
Isomeric SMILES | CCN1CCN(CC1)CC2=C(C=C(C=C2)NC(=O)NC3=CC=C(C=C3)OC4=NC=NC(=C4)NC)C(F)(F)F |
PubChem CID | 11409972 |
Molecular Weight | 529.56 |
CAS Registry No. | 630124-46-8 |
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DiscoveRx TREEspot | AST-487| |
PubChem CID | 11409972 |
ChEMBL Ligand | CHEMBL574738 |
Enter Lot Number to search for COA:
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Lot Number | Certificate Type | Date | Item |
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I2217134 | Certificate of Analysis | Jul 19, 2024 | A413573 |
I2217148 | Certificate of Analysis | Jul 19, 2024 | A413573 |
I2217162 | Certificate of Analysis | Jul 19, 2024 | A413573 |
I2217164 | Certificate of Analysis | Jul 19, 2024 | A413573 |
I2217165 | Certificate of Analysis | Jul 19, 2024 | A413573 |
I2217167 | Certificate of Analysis | Jul 19, 2024 | A413573 |
Solubility | Solubility (25°C) In vitro DMSO: 100 mg/mL (188.83 mM); Ethanol: 33 mg/mL (62.31 mM); Water: Insoluble; |
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1. Akeno-Stuart N, Croyle M, Knauf JA, Malaguarnera R, Vitagliano D, Santoro M, Stephan C, Grosios K, Wartmann M, Cozens R et al.. (2007) The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells.. Cancer Res, 67 (14): (6956-64). [PMID:17638907] |
2. Weisberg E, Roesel J, Bold G, Furet P, Jiang J, Cools J, Wright RD, Nelson E, Barrett R, Ray A et al.. (2008) Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells.. Blood, 112 (13): (5161-70). [PMID:18820131] |