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Alectinib | Potent and selective ALK inhibitor

Alectinib (1256580-46-7) is a potent (IC50 = 1.9 nM) and highly selective ALK inhibitor.1 It blocked phosphorylation of both native ALK and the L1196M, C1156Y, and F1174L mutants. Alectinib has also been shown to inhibit RET kinase (IC50 = 4.8 nM), the RET gatekeeper mutations V804L and V804M, and inhibited the growth of RET fusion positive cells.2 Alectinib is clinically useful in the treatment of ALK-positive Non-Small Cell Lung Cancer. It effectively suppressed cell proliferation and induced apoptosis in a mouse neuroblastoma xenograft.3

References/Citations
1) Sakamoto et al. (2011), CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant; Cancer Cell, 19 679
2) Kodama et al. (2014), Alectinib Shows Potent Antitumor Activity against RET-Rearranged Non-Small Cell Lung Cancer., Mol. Cancer Ther. 13 2910
3) Lu et al. (2017), 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, 400 61

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Catalog#  10-4793-0005

$60.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1256583-46-7
Catalog Number:
10-4793
Activity:
Potent and selective ALK inhibitor
Chemical Name:
9-Ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
Alternate Name:
CH5424802
Molecular Weight:
482.62
Molecular Formula:
C30H34N4O2
Solubility:
Soluble in DMSO (up to 5 mg/ml with warming).
Physical Properties:
White solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions are not stable and should be prepared fresh daily.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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