CH5424802

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 10mM*1mL (in DMSO)
ArtNr HY-13011-10mM
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Synonyms
Alectinib, AF-802, CH 5424802, CH-5424802, AF802, AF 802
CAS No.
1256580-46-7
Purity
>98%
MW
4826165
Formula
C30H34N4O2
Solubility
DMSO: 6.2 mg/mL (Need warming)
Biological Description
CH5424802 is a potent, selective, and orally available ALK inhibitor with IC50 of 1.9 nM, the dissociation constant (KD) value for ALK in an ATP-competitive manner is 2.4 nM using a competition-binding assay.
IC50 & Target: IC50: 1.9 nM(ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)[1]

Kd: 2.4 nM (ALK)[1]
In Vitro: CH5424802 prevents autophosphorylation of ALK in NCI-H2228 NSCLC cells expressing EML4-ALK, and CH5424802 also results in substantial suppression of phosphorylation of STAT3 and AKT, but not of ERK1/2[1]. CH5424802 shows high kinase selectivity and strong anti-proliferative activity against KARPAS-299 with an IC50 value of 3 nM[2].
In Vivo: In the NCI-H2228 model, once-daily oral administration of CH5424802 results in dose-dependent tumor growth inhibition (ED50=0.46 mg/kg) and tumor regression. Treatment of 20 mg/kg CH5424802 shows rapid tumor regression (168% tumor growth inhibition; p<0.001), the tumor volume in any mouse is <30 mm3 after 11 days of treatment (at day 28), a potent antitumor effect is maintained, and tumor re-growth dpes not occur throughout the 4-week drug-free period[1]. Oral administration of CH5424802 at 20 mg/kg displays significant tumor regression without body weight loss in an established ALK fusion gene-positive NSCLC xenograft model in mice[2]. CH5424802 (Alectinib) at 60 mg/kg causes tumor regression against EML4-ALK-positive NCI-H2228 xenograft model and decreases the levels of phosphorylated ALK in this model. In addition, in mice at dose levels up to 60 mg/kg of CH5424802, there is no body weight loss, no significant change in peripheral blood cell count, no elevations of aspartate aminotransferase or alanine aminotransferase, and no substantial change in electrolytes. Oral administration of CH5424802 at 60 mg/kg for 4 days results in significant tumor regression seen in the luminescence signal[3].
Publications
Cancer Discov. 2016 Oct; 6(10):1118-1133.
Science. 2014 Oct 3; 346(6205):1255784.
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Journal
Lu J, et al. The second-generation ALK inhibitor alectinib effectively induces apoptosis in human neuroblastoma cells and inhibits tumor growth in a TH-MYCN transgenic neuroblastoma mouse model. Cancer Lett. 2017 Aug 1; 400:61-68.
Menge: 10mM*1mL (in DMSO)
Lieferbar: In stock
Listenpreis: 127,14 €
Rabatt: -10,0%
Preis: 114,43 €
Sie sparen: 12,71 €
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