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TH9619

Chemical Structure : TH9619

CAS No.: 2379556-22-4

TH9619 (TH-9619)

货号: PC-72940Not For Human Use, Lab Use Only.

TH9619 (TH-9619) is a potent and selective inhibitor of folate metabolism enzyme MTHFD2 with IC50 of 47 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 451.371
分子式 C17H18FN7O7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[[5-[[2-(2,4-Diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)acetyl]amino]-3-fluoro-2-pyridinyl]carbonyl]-L-glutamic acid

参考文献

1. Nadilly Bonagas, et al. Nat Cancer. 2022 Feb;3(2):156-172.

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