CH5424802

For research use only. Not for therapeutic Use.

  • CAT Number: A000528
  • CAS Number: 1256580-46-7
  • Molecular Formula: C₃₀H₃₄N₄O₂
  • Molecular Weight: 482.62
  • Purity: ≥95%
Inquiry Now

Alectinib(cas 1256580-46-7)  is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo. CH5424802 inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors, and blocked EML4-ALK L1196M-driven cell growth. Alectinib was approved in Dec. 2015.


Catalog Number A000528
CAS Number 1256580-46-7
Synonyms

Alectinib free base; 9-ethyl-6,6-dimethyl-8-(4-morpholinopiperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile

Molecular Formula C₃₀H₃₄N₄O₂
Purity ≥95%
Target ALK
Solubility Soluble in DMSO, not in water
Storage 3 years -20C powder
InChI InChI=1S/C30H34N4O2/c1-4-20-16-23-24(17-26(20)34-9-7-21(8-10-34)33-11-13-36-14-12-33)30(2,3)29-27(28(23)35)22-6-5-19(18-31)15-25(22)32-29/h5-6,15-17,21,32H,4,7-14H2,1-3H3
InChIKey KDGFLJKFZUIJMX-UHFFFAOYSA-N
SMILES CCC1=C(C=C2C(=C1)C(=O)C3=C(C2(C)C)NC4=C3C=CC(=C4)C#N)N5CCC(CC5)N6CCOCC6
Reference

1: Gainor JF, Shaw AT. J-ALEX: alectinib versus crizotinib in ALK-positive lung
cancer. Lancet. 2017 May 10. pii: S0140-6736(17)31074-7. doi:
10.1016/S0140-6736(17)31074-7. [Epub ahead of print] PubMed PMID: 28501139. <br />
2: Morcos PN, Parrott N, Banken L, Timpe C, Lindenberg M, Guerini E, Dall G,
Bogman K, Sturm C, Zeaiter A, Martin-Facklam M, Phipps A. Effect of the Wetting
Agent Sodium Lauryl Sulfate on the Pharmacokinetics of Alectinib: Results From a
Bioequivalence Study in Healthy Subjects. Clin Pharmacol Drug Dev. 2017
May;6(3):266-279. doi: 10.1002/cpdd.299. Epub 2016 Oct 3. PubMed PMID: 27545871.<br />
3: Carlson JJ, Canestaro W, Ravelo A, Wong W. The cost-effectiveness of alectinib
in anaplastic lymphoma kinase-positive (ALK+) advanced NSCLC previously treated
with crizotinib. J Med Econ. 2017 Mar 23:1-7. doi: 10.1080/13696998.2017.1302453.
[Epub ahead of print] PubMed PMID: 28332433.<br />
4: Morcos PN, Bogman K, Hubeaux S, Sturm-Pellanda C, Ruf T, Bordogna W, Golding
S, Zeaiter A, Abt M, Balas B. Effect of alectinib on cardiac electrophysiology:
results from intensive electrocardiogram monitoring from the pivotal phase II
NP28761 and NP28673 studies. Cancer Chemother Pharmacol. 2017 Mar;79(3):559-568.
doi: 10.1007/s00280-017-3253-5. Epub 2017 Feb 27. PubMed PMID: 28243683. <br />
5: Morcos PN, Yu L, Bogman K, Sato M, Katsuki H, Kawashima K, Moore DJ, Whayman
M, Nieforth K, Heinig K, Guerini E, Muri D, Martin-Facklam M, Phipps A.
Absorption, distribution, metabolism and excretion (ADME) of the ALK inhibitor
alectinib: results from an absolute bioavailability and mass balance study in
healthy subjects. Xenobiotica. 2017 Mar;47(3):217-229. doi:
10.1080/00498254.2016.1179821. Epub 2016 May 16. PubMed PMID: 27180975.<br />
6: Lockney NA, Wu AJ. Alectinib for the management of ALK-positive non-small cell
lung cancer brain metastases. J Thorac Dis. 2017 Feb;9(2):E152-E154. doi:
10.21037/jtd.2017.02.05. PubMed PMID: 28275502; PubMed Central PMCID: PMC5334091. <br />
7: Iwama E, Goto Y, Murakami H, Harada T, Tsumura S, Sakashita H, Mori Y,
Nakagaki N, Fujita Y, Seike M, Bessho A, Ono M, Okazaki A, Akamatsu H, Morinaga
R, Ushijima S, Shimose T, Tokunaga S, Hamada A, Yamamoto N, Nakanishi Y, Sugio K,
Okamoto I. Alectinib for Patients with ALK Rearrangement-Positive Non-Small Cell
Lung Cancer and a Poor Performance Status (Lung Oncology Group in Kyushu 1401). J
Thorac Oncol. 2017 Feb 24. pii: S1556-0864(17)30123-5. doi:
10.1016/j.jtho.2017.02.012. [Epub ahead of print] PubMed PMID: 28238961.

Request a Quote