Alectinib-d6

Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

Product Specifications

CAS Number

[1616374-19-6]

Product Name Alternative

CH5424802-d6; RO5424802-d6; AF802-d6

UNSPSC

12352005

Target

Anaplastic lymphoma kinase (ALK) ; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

Others; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Purity

98.05

Solubility

10 mM in DMSO

Smiles

O=C1C2=C(NC3=CC(C#N)=CC=C32)C(C([2H])([2H])[2H])(C4=CC(N5CCC(N6CCOCC6)CC5)=C(CC)C=C41)C([2H])([2H])[2H]

Molecular Formula

C30H28D6N4O2

Molecular Weight

488.65

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29 (11) :2214-2222.|[3]Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19 (5), 679-690.