Olafertinib

Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) . Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies[1][2].

Product Specifications

CAS Number

[1660963-42-7]

Product Name Alternative

CK-101; RX518

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/EGFR-IN-3.html

Purity

99.51

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

OCCN1CCN(C2=C(F)C(F)=C(NC3=NC=C4C(C(C5=CC(NC(C=C)=O)=CC=C5)=CC=C4)=N3)C=C2)CC1

Molecular Formula

C29H28F2N6O2

Molecular Weight

530.57

Precautions

H302, H315, H319, H335

References & Citations

[1]Johnson, M. et al., (2018) OA02.05 CK-101 (RX518), a Third Generation Mutant-Selective Inhibitor of EGFR in NSCLC: Results of an Ongoing Phase I/II Trial. Journal of Thoracic Oncology, Volume 13, Issue 10, S323.|[2]Xiangping Qian, et al., Abstract 2078: CK-101 (RX518), a mutant-selective inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Res 1 July 2017; 77 (13_Supplement) : 2078.