Sapitinib

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 5mg
ArtNr HY-13050-5mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
AZD-8931
CAS No.
848942-61-0
Purity
>98%
MW
4739277
Formula
C23H25ClFN5O3
Solubility
DMSO: >= 33 mg/mL
Biological Description
Sapitinib(AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM respectively.
IC50 value: 4/3/4 nM(EGFR/ERBB2/ERBB3) [1]
Target: EGFR inhibitor
in vitro: ZD8931 shows different potency to NSCLC and SCCHN cell lines. AZD8931 has high sensitivity to PC-9 cells (EGFR activating mutation) with GI50 of 0.1 nM and low activity to NCI-1437 cells with GI50 above 10 uM. AZD8931 exhibits more potency against phospho-EGFR, phospho-erbB2 and phospho-erbB3 than either lapatinib or gefitinib in PE/CA-PJ41, PE/CA-PJ49, DOK and FaDu cells [1]. AZD8931 significantly suppressed cell growth of IBC cells and induced apoptosis of human IBC cells in vitro [2].
in vivo: AZD8931 reveals antitumor activity in BT474c, Calu-3, LoVo, FaDu and PC-9 xenografts. AZD8931 could reduce p-Akt, Ki67 expression and p-ERK in BT474c xenografts following acute treatment. AZD8931 also causes induction of the M30 apoptosis marker. Furthermore, AZD8931 shows greater proapoptotic effect compared with gefitinib and lapatinib in LoVo xenografts [1]. AZD8931 monotherapy inhibited xenograft growth and the combination of paclitaxel + AZD8931 was demonstrably more effective than paclitaxel or AZD8931 alone treatment at delaying tumor growth in vivo in orthotopic IBC models [2]. AZD8931 exhibited good pharmacokinetics in preclinical species and showed superior activity in the LoVo tumor growth efficacy model compared to close analogues [3].
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Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 5mg
Lieferbar: In stock
Listenpreis: 108,93 €
Preis: 108,93 €
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