Alectinib

SKU: orb1226665

Description

A potent, selective ALK inhibitor with IC50 of 1.9 nM; shows high selectivity versus KDR, KIT and MET (IC50>1,400 nM); exhibits anti-proliferative activity against NPM-ALK-positive cellline KARPAS-299 with IC50 of 3 nM; also inhibits mutant ALK F1174L and R1275Q with IC50 of 1 nM and 3.5 nM respectively; orally active.Lung Cancer Approved(In Vitro):Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT.Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner.(In Vivo):Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1256580-46-7
• MW: 482.6165
• Purity: >98% (HPLC)
• Formula: C₃₀H₃₄N₄O₂
• SMILES: CCC1=C(C=C2C(=C1)C(=O)C1=C(NC3=C1C=CC(=C3)C#N)C2(C)C)N1CCC(CC1)N1CCOCC1
• Target: ALK
• Solubility: DMSO: 6.2 mg/mL (Need warming)

Bioactivity

• In Vivo:
  Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed. Animal model: SCID or nude mice bearing NCI-H2228 cells. Dosage: 0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg. Administration: Oral administration; once daily; for 11 days. Result: Resulted in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression.
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• In Vitro:
  Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT. Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner. Western blot analysis. Cell line: NCI-H2228 cells. Concentration: 0 nM, 10 nM, 100 nM, 1000 nM. Incubation time: 2 hours. Result: Inhibition of ALK phosphorylation and signal transduction. Cell Viability Assay Cell line: HCC827, A549, or NCIH522 cells. Concentration: 0-1000 nM. Incubation time: 5 days. Result: Reduced cell activity in a dose-dependent manner.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CH5424802 | AF-802 | CH 5424802 | AF802 | AF 802

Quick Database Links

Gene Symbol

ALK