LY 345899

SKU: orb1219692

Description

LY 345899 is a Folate analog and is a methylenetetrahydrofolate dehydrogenase and MTHFD2 inhibitor (IC50: 96 nM and 663 nM, respectively and a Ki: 18 nM for MTHFD1).

Key Properties

• CAS Number: 10538-99-5
• MW: 471.42
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₁N₇O₇
• SMILES: Nc1nc(=O)c2N3C(CN(C3=O)c3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)CNc2[nH]1
• Target: MTHFD1
• Solubility: DMSO:125 mg/mL (265.16 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  LY345899 (Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks) shows potent antitumor activity and displays therapeutic activity against CRC In vivo. Animal model: SW620 or PDX-based BABL/c nude colorectal cancer (CRC) model. Dosage: 5-10 mg/kg. Administration: Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks. Result: Displayed lower cell proliferation indices and higher cell apoptosis. Exhibited no statistically significant weight loss or other signs of acute or delayed toxicity in mice.
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• In Vitro:
  LY 345899 could suppress the MTHFD enzyme in the cytoplasm and mitochondria. LY 345899 could disturb the NADPH and redox homeostases and accelerate cell death under oxidative stress, such as hypoxia, or causing in vitro anchorage independence and in vivo impaired tumor growth and metastasis.
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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

MTHFD1