Adavosertib

SKU: orb1223527

Description

A potent and selective small-molecule inhibitor of Wee1 kinase with IC50 of 5.2 nM; exhibits ATP-competitive and highly selective against other serine/threonine or tyrosine kinases; inhibits phosphorylation of CDC2 at Tyr15 in cells; potentiates tumor growth inhibition in vivo.Lung Cancer Phase 2 Clinical(In Vitro):Adavosertib (MK-1775) enhances the cytotoxic effects of 5-FU in p53-deficient human colon cancer cells. Adavosertib (MK-1775) inhibits CDC2 Y15 phosphorylation in cells, abrogates DNA damaged checkpoints induced by 5-FU treatment, and causes premature entry of mitosis determined by induction of Histone H3 phosphorylation. Adavosertib (MK-1775) abrogates the radiation-induced G2 block in p53-defective cells but not in p53 wild-type lines. The combination of NSC 613327 with Adavosertib (MK-1775) produces robust anti-tumor activity and remarkably enhances tumor regression response (4.01 fold) compared to NSC 613327 treatment in p53-deficient tumors.(In Vivo):In vivo, Adavosertib (MK-1775) potentiates the anti-tumor efficacy of 5-FU at tolerable doses. Adavosertib (MK-1775) (60 mg/kg twice daily, p.o.) enhances H1299 xenograft tumor response to fractionated radiotherapy. Adavosertib (MK-1775) (30 mg/kg. p.o.) regresses tumor growth in PANC198, PANC215 and PANC185 as compared to GEM treated mice.

Key Properties

• CAS Number: 955365-80-7
• MW: 500.5954
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₂N₈O₂
• SMILES: O=C1N(CC=C)N(C2=NC(C(C)(O)C)=CC=C2)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=NC=C31
• Target: Wee1
• Solubility: 10 mM in DMSO

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

AZD-1775 | MK-1775

Quick Database Links

Gene Symbol

Wee1