[CAS NO. 1256589-74-8]  Alectinib (CH5424802) hydrochloride

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PRODUCTS SPECIFICATIONS [1256589-74-8]

Store
Catalog
SLK-S5232
Brand
Selleck
CAS
1256589-74-8

DESCRIPTION [1256589-74-8]

Overview

MDLMFCD27987893
Molecular Weight519.08
Molecular FormulaC30H34N4O2.HCl
SMILESO=C1C2=C(C(C)(C)C=3C1=CC(CC)=C(C3)N4CCC(CC4)N5CCOCC5)NC=6C2=CC=C(C#N)C6.Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.9265 mL9.6324 mL19.2649 mL
5 mM---
10 mM---
50 mM---

Description

Alectinib (AF802, CH5424802, RO5424802, RG-7853) is a second generation oral drug that selectively inhibits the activity of tyrosine kinase.

Targets

ALK [1]
(Cell-free)
1.9 nM

In vitro

Alectinib inhibits ALK with an IC50 value of 1.9 nmol/L and shows higher selectivity for ALK than for a number of other serine/tyrosine kinases. It also inhibits the ALK gatekeeper mutation L1196M with an IC50 of 1.56 nmol/L. Alectinib is effective with crizotinib-resistant ALK mutations L1196M, F1174L, R1275Q and C1156Y. In the KARPAS-299 (lymphoma), NB-1 (neuroblastoma) and NCI-H2228 (lung cancer) ALK-positive cell lines, alectinib inhibits cell proliferation with IC50 values of 3, 4.5 and 53 nmol/L, respectively.

In vivo

Alectinib dose-dependently inhibits EML4-ALK positive NCI-H2228 xenograft model at doses ranging from 2 to 20 mg/kg p.o., q.d. Significant efficacy is also achieved in the EML4-ALK L1196M-driven tumors. It has antitumor activity against cancers with ALK gene alterations.


Synonyms

5H-Benzo[b]carbazole-3-carbonitrile, 9-ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-, hydrochloride (1:1)
Alectinib hydrochloride
Alecensa