Vergleich

AZD5438 Europäischer Partner

ArtNr S2621-10mM
Hersteller Selleckchem
CAS-Nr. 602306-29-6
Menge 10 mM/1 ml
Quantity options 10 mg 1 g 10 g 10 mM/1 ml 200 mg 50 mg 5 g
Kategorie
Typ Inhibitors
Specific against other
Smiles CC1=NC=C(N1C(C)C)C2=NC(=NC=C2)NC3=CC=C(C=C3)S(=O)(=O)C
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias 602306-29-6 '
Similar products AZD5438
Lieferbar
Manufacturer - Targets
CDK9, CDK2, CDK1
Storage Conditions
2 years -80 in solvent
Molecular Weight
371, 46
Administration
Administered via p.o.
Animal Models
MCF-7, HCT-116, A549, and IM-9 cells are injected s.c. into the Swiss nude mice and nude rats.
Cell lines
MCF-7, HCT-116, A549, and IM-9
Clinical Trials
Study on AZD5438 has been completed in Phase I clinical trials in patients with Advanced Solid Malignancies.
Concentrations
0 to 10 uM
Dosages
<=100 mg/kg
Formulation
AZD5438 is dissolved in hydroxy-propyl-methyl-cellulose.
IC50
16 nM [1], 16 nM [1], 16 nM [1], 16 nM [1], 16 nM [1], 16 nM [1]
In vitro
AZD5438 exhibits the potent inhibitory effect on activity of cyclin-dependent kinases including cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, cyclin D3-cdk6, and cyclin T-cdk9 with IC50 of 6 nM, 45 nM, 16 nM, 21 nM, and 20 nM, respectively. Besides, AZD5438 also inhibits the kinase activity of p25-cdk5 and glycogen synthase kinase 3beta with IC50 of 14 nM and 17 nM, respectively. [1] AZD5438 induces cell cycle arrest by inhibiting phosphorylation of cdk-dependent substrates, and exhibits the broad antiproliferative activity against a range of tumor cell lines including lung, colorectal, breast, prostate, and hematologic tumors with IC50 ranging from 0.2 uM (MCF-7) to 1.7 uM (ARH-77). [1]
In vivo
In vivo, oral treatment of AZD5438 leads to statistically significant inhibition against the growth of human tumor xenografts derived from a wide range of different cancer types including breast, colon, lung, prostate, and ovarian with maximum TGI ranging from 38% to 153%. [1] In the SW620 xenograft model, AZD5438 causes the inhibition of several cell cycle proteins such as, phH3, phosphonucleolin, PP1a, and several phospho-pRb epitopes in a dose-dependent manner. [1]
Incubation Time
48 hours or 72 hours
Method
AZD5438 is tested against solid tumor cell lines. Briefly, cells are incubated for 48 hours with AZD5438 at a range of concentrations. At the end of incubation, the cells are pulsed with 5-bromo-2 -deoxyuridine (BrdUrd) and the amount of DNA synthesis is measured. The IC50 for inhibition of proliferation is specifically determined independently of cell death. Multiple myeloma cell lines are seeded into 96-well plates in RPMI 1640 supplemented with 10% FCS and glutamine and dosed with AZD5438 for 72 hours. Cell growth is measured using AlamarBlue and GI50 values are calculated with reference to pretreatment control values.
Solubility (25C)
DMSO 74 mg/mL, Water <1 mg/mL, Ethanol 74 mg/mL
Information
AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It is less potent to CDK5/6 and also inhibits GSK3β.
Chemical Name
4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)-N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine
Features
AZD5438 is a potent inhibitor of cyclin-dependent kinase (cdk) 1, 2, and 9.

Hinweis: Die dargestellten Informationen und Dokumente (Bedienungsanleitung, Produktdatenblatt, Sicherheitsdatenblatt und Analysezertifikat) entsprechen unserem letzten Update und sollten lediglich der Orientierung dienen. Wir übernehmen keine Garantie für die Aktualität. Für spezifische Anforderungen bitten wir Sie, uns eine Anfrage zu stellen.

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

Menge: 10 mM/1 ml
Lieferbar: In stock
lieferbar

Vergleichen

Auf den Wunschzettel

Angebot anfordern

Lieferzeit anfragen

Technische Frage stellen

Bulk-Anfrage stellen

Fragen zum Produkt?