APS6-45

SKU: orb1218429

Description

APS6-45 inhibits RAS/MAPK signaling and exhibits anti-tumor activity.

Key Properties

• CAS Number: 2188236-41-9
• MW: 548.4
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₆F₈N₄O₃
• SMILES: O=C(NC)C1=NC=CC(OC2=CC=C(NC(NC3=CC(C(C(F)(F)F)(F)C(F)(F)F)=CC=C3F)=O)C=C2)=C1
• Target: p38 MAPK
• Solubility: DMSO:240mg/mL (437.67mM)

Bioactivity

• In Vivo:
  APS6-45 (10 mg/kg; p.o. daily for 30 d) inhibits growth of TT tumors in mice and does not affect body weight. APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice. APS6-45 (20 mg/kg; a single p.o.) exhibits long half-life (5.6 h), Cmax (9.7 μM) and AUC0-24 (123.7 μM h) in mice. Animal model: Female nude mice (6 weeks) are implanted with TT cells. Dosage: 10 mg/kg. Administration: p.o. daily for 30 days. Result: Led to partial or complete responses in 75% and was well tolerated. Animal model: Male ICR mice (6 weeks of age). Dosage: 20 mg/kg (Pharmacokinetic Analysis). Administration: A single p.o. Result: T1/2 = 5.6 h, Cmax = 9.7 μM, AUC0-24 = 123.7 μM h.
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• In Vitro:
  APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay. APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1.
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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

Quick Database Links

Gene Symbol

p38 MAPK