I. Basic Information

• Product Name: Ceritinib

• CAS Number: 1032900-25-6

• Molecular Formula: C28H36ClN5O3S

• Molecular Weight: 558.13514 (or 558.14)

• Appearance: White to off-white powder

• Purity: ≥98% (or 99.98%, depending on product specifications)

II. Physical and Chemical Properties

• Density: 1.3±0.1 g/cm3

• Boiling Point: Multiple boiling points exist, such as 720.7±70.0 °C at 760 mmHg or 1184.5 °C (may vary due to testing conditions and methods)

• Flash Point: 389.6±35.7 °C

• Solubility: Soluble in DMSO

• Log P: 5.62 or 5.03 (may vary due to testing methods and conditions)

III. Biological Activity and Target

• Target: ALK (Anaplastic Lymphoma Kinase), Insulin Receptor, IGF-1R (Insulin-like Growth Factor 1 Receptor), etc.

• IC50 Value: The IC50 value for ALK is 0.2 nM (or 200 pM), demonstrating potent and specific inhibition; it also has inhibitory effects on other kinases such as InsR and IGF-1R, but with relatively high selectivity.

IV. Application Fields and Indications

• Application Fields: Primarily used in cancer treatment research and drug development.

• Indications: Suitable for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib.

V. Pharmacokinetic Characteristics

• Oral Bioavailability: Exhibits excellent pharmacokinetic properties in rodents and non-rodents, with oral bioavailability >50%.

• Tumor Growth Inhibition: Demonstrates dose-dependent tumor growth inhibition in multiple animal models and can achieve complete tumor regression in some models.