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LDK378 CAS: 1032900-25-6

Category: Inhibitors
Product Name: LDK378
Cat No: I000197
CAS No: 1032900-25-6
Synonyms: 5-chloro-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine
Molecular Formula: C28H36ClN5O3S
Molecular Weight: 558.1
SMILES: CC(C=C(NC1=NC=C(Cl)C(NC2=CC=CC=C2S(C(C)C)(=O)=O)=N1)C(OC(C)C)=C3)=C3C4CCNCC4
InChIKey: VERWOWGGCGHDQE-UHFFFAOYSA-N
Solubility: DMSO: ≥ 5.6 mg/mL (Need ultrasonic)
Target: ALK
IC50: 0.2 nM [1]
Storage: powder
CAS 1032900-25-6,LDK378
  • Description

LDK378(Ceritinib) is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.
IC50 Value: 0.2 nM [1]
Target: ALK
in vitro: LDK378 shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells [1].
in vivo: LDK378 is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. LDK378 has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. LDK378 exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. LDK378 induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. LDK378 shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg [1].

  • Spec


Assay:≥98%
Appearance:A crystalline solid

  • References


[1]. Marsilje TH, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013, Jun 6.


price inquiry for CAS:1032900-25-6, Product:LDK378