Alectinib-d8

• UNSPSC Description:

  Alectinib-d8 is the 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].

• Target Antigen:

  Anaplastic lymphoma kinase (ALK); Isotope-Labeled Compounds

• Type:

  Isotope-Labeled Compounds

• Related Pathways:

  Others;Protein Tyrosine Kinase/RTK

• Field of Research:

  Cancer

• Solubility:

  10 mM in DMSO

• Smiles:

  N#CC1=CC2=C(C3=C(N2)C(C)(C4=CC(N5CCC(CC5)N6C([2H])([2H])C([2H])([2H])OC([2H])([2H])C6([2H])[2H])=C(C=C4C3=O)CC)C)C=C1

• Molecular Weight:

  490.67

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. |[2]Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690.|[3]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.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported

• CAS Number:

  1256585-15-5