Free shipping on all orders over $ 500

CH5424802 HCl

Cat. No. M4811
CH5424802 HCl Structure
Synonym:

AF802 HCl; Alectinib Hydrochloride

Size Price Availability Quantity
10mg USD 60  USD60 In stock
25mg USD 85  USD85 In stock
50mg USD 110  USD110 In stock
100mg USD 190  USD190 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

CH5424802 (AF802) is a potent, selective, and orally available ALK inhibitor. Anaplastic lymphoma kinase (ALK) receptor tyrosine kinase is considered an attractive therapeutic target for human cancers. CH5424802 (AF802) 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. CH5424802 also blocked EML4-ALK L1196M-driven cell growth.

Chemical Information
Molecular Weight 519.08
Formula C30H35ClN4O2
CAS Number 1256589-74-8
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kinoshita K, et al. Bioorg Med Chem. Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).

[2] Sakamoto H, et al. Cancer Cell. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.

Related ALK Products
NVL-655

NVL-655 is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 has an IC50 of 2.7 nM. It can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC).

APG-2449

APG-2449 is an orally active, potent ALK/ROS1/FAK inhibitor with anti-tumor activity in a mouse model of non-small cell lung cancer (NSCLC).

ALK2-IN-5

ALK2-IN-5, pyrazolopyrimidine compound, is an ALK2 inhibitor.

J-1048

J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor.

CPD-1224

CPD-1224 is an orally active derivative of ALK inhibitors to cereblon ligands.

  Catalog
Abmole Inhibitor Catalog




Keywords: CH5424802 HCl, AF802 HCl; Alectinib Hydrochloride supplier, ALK, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.