AST-1306

SKU: orb1227062

Description

AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases,(In Vitro):AST1306 tosylate (AST-1306 (TsOH); 0.19-6.25 μM; 72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells.AST1306 tosylate inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 tosylate dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells.AST1306 tosylate (0.1, 0.5, 1.0, 5.0 μM) can dramatically inhibit the growth of both tumor cells on soft agar, and SK-OV-3 cells exhibited much more sensitivity than that of A549 cells.AST1306 tosylate (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families.AST1306 tosylate potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50 value of 12±2 nmol/L.(In Vivo):AST1306 tosylate (AST-1306 (TsOH); p.o.; 25-100 mg/kg; twice daily; for 28 days) causes a dramatic suppression of tumor growth in SK-OV-3 and Calu-3 xenograft models.

Key Properties

• CAS Number: 1050500-29-2
• MW: 621.08
• Purity: >98% (HPLC)
• Formula: C₃₁H₂₆ClFN₄O₅S
• SMILES: CC1=CC=C(C=C1)S(O)(=O)=O.FC1=CC(COC2=CC=C(NC3=C4C=C(NC(=O)C=C)C=CC4=NC=N3)C=C2Cl)=CC=C1 |c:3,5,22,31,34,36,39,42,44,t:1,12,17,19,24|
• Target: EGFR
• Solubility: DMSO:124 mg/mL (199.65 mM); Ethanol:<1 mg/mL (<1 mM); Water：<1 mg/mL (<1 mM)

Bioactivity

• In Vivo:
  AST1306 tosylate (AST-1306 (TsOH); p.o. ; 25-100 mg/kg; twice daily; for 28 days) causes a dramatic suppression of tumor growth in SK-OV-3 and Calu-3 xenograft models. Animal model: Nude mice with SK-OV-3 and Calu-3 tumors. Dosage: 25, 50, 100 mg/kg. Administration: p.o. ; twice daily; for 28 days. Result: Caused a dramatic suppression of tumor growth.
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• In Vitro:
  AST1306 tosylate (AST-1306 (TsOH); 0.19-6.25 μM; 72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells. AST1306 tosylate inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 tosylate dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells. AST1306 tosylate (0.1, 0.5, 1.0, 5.0 μM) can dramatically inhibit the growth of both tumor cells on soft agar, and SK-OV-3 cells exhibited much more sensitivity than that of A549 cells. AST1306 tosylate (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families. AST1306 tosylate potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50 value of 12±2 nmol/L.
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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

EGFR