Cas No.: | 2379556-22-4 |
Chemical Name: | TH9619 |
Synonyms: | L-Glutamic acid, N-[[5-[[2-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)acetyl]amino]-3-fluoro-2-pyridinyl]carbonyl]- |
SMILES: | C(O)(=O)[C@H](CCC(O)=O)NC(C1=NC=C(NC(CC2C(=O)NC(N)=NC=2N)=O)C=C1F)=O |
Formula: | C17H18FN7O7 |
M.Wt: | 451.365926265717 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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. |