TH9619

SKU: orb1910687

Description

TH9619 (TH-9619) is a potent and selective inhibitor of folate metabolism enzyme MTHFD2 with IC50 of 47 nM.TH9619 demonstrated efficacy on HL-60 cell viability with EC50 of 11 nM.TH9619 potently inhibits related MTHFD proteins MTHFD2L and MTHFD1-(DC) with IC50 of 47 and 16 nM, respectively.TH9619 displays high potency and cancer selectivity in AML models. induce thymine-less DNA damage and apoptosis, causes uracil misincorporation into DNA, sensitize cancer cells to ATR-signaling blockade.TH9619 impairs cancer progression in vivo.TH9619 displays high selectivity toward binding and stabilizing MTHFD2 over other common folate metabolism targets such as DHFR, thymidylate synthase (TYMS), serine hydroxymethyltransferase (SHMT) 1 and SHMT2.

Key Properties

• CAS Number: [2379556-22-4]
• MW: 451.365926265717
• Formula: C₁₇H₁₈FN₇O₇
• SMILES: C(O)(=O)[C@H](CCC(O)=O)NC(C1=NC=C(NC(CC2C(=O)NC(N)=NC=2N)=O)C=C1F)=O

Storage & Handling

• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only