Vergleich

AST 487

ArtNr CS-0779-5mg
Hersteller ChemScene
Menge 5mg
Kategorie
Typ Molecules
Specific against other
ECLASS 10.1 32169090
ECLASS 11.0 32169090
UNSPSC 12000000
Similar products 630124-46-8
Lieferbar
Alternative Names
NVP-AST 487
CAS
630124-46-8
Purity
>98%
Formula
C26H30F3N7O2
MWt
529.56
Solubility
DMSO : >= 100 mg/mL (188.84 mM)
Clinical Information
No Development Reported
Pathway
Protein Tyrosine Kinase/RTK; Protein Tyrosine Kinase/RTK; Protein Tyrosine Kinase/RTK; Protein Tyrosine Kinase/RTK; Protein Tyrosine Kinase/RTK
Target
VEGFR; Bcr-Abl; FLT3; c-Kit; RET
Biological Activity
AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM. IC50 & Target: IC50: 880 nM (RET), 170 nM (KDR), 790 nM (Flt-4), 500 nM (c-Kit), 520 nM (Flt-3), 20 nM (Abl)[1] In Vitro: A number of other kinases are also similarly inhibited by AST 487 (NVP-AST487) in the in vitro kinase assays, including KDR (IC50=170 nM), Flt-4 (IC50=790 nM), Flt-3 (IC50=520 nM), c-Kit (IC50=500 nM), and c-Abl (IC50=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/GFRalpha1 and persephin-induced calcitonin mRNA are markedly inhibited by coincubation with 100 nM of AST 487 in MTC-M cells[1]. AST 487 is a novel, mutant FLT3 inhibitor. AST 487 is tested in biochemical assays for inhibition of Flt-3 kinase activity. The Ki is determined to be 0.12 uM. Besides Flt-3, NVP-AST487 inhibits RET, KDR, c-Kit, and c-Abl kinase with IC50 values below 1 uM. Treatment of FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells with AST 487 potently inhibits cellular proliferation (IC50<5 nM). AST 487 treatment of FLT3-ITD-Ba/F3 cells with 0.01 uM AST 487 results in complete cell killing compare with approximately 50% killing of AML patient samples at the same concentration[2]. In Vivo: After a single oral administration of 15 mg/kg of AST 487 to OF1 mice, a mean peak plasma level (Cmax) of 0.505+/-0.078 uM 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 Clast of 21+/-4 nM at 24 h. The oral bioavailability is calculated to be 9.7% with a t1/2 terminal elimination of 1.5 h[1].

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Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Menge: 5mg
Lieferbar: In stock
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