AGF347 | SHMT2 inhibitor | Probechem Biochemicals

Chemical Structure : AGF347

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AGF347 (AGF-347)

货号: PC-72124Not For Human Use, Lab Use Only.

AGF347 (AGF-347) is a small molecule inhibitor targeting mitochondrial C1 metabolism at SHMT2 (in vitro Ki=2.19 uM), also directly targers the purine biosynthetic enzymes GARFTase (Ki=3.13 uM) and AICARFTase (Ki=3.72 uM), and SHMT1 (Ki=2.91 uM).

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生物&药学活性

AGF347 (AGF-347) is a small molecule inhibitor targeting mitochondrial C1 metabolism at SHMT2 (in vitro Ki=2.19 uM), also directly targers the purine biosynthetic enzymes GARFTase (Ki=3.13 uM) and AICARFTase (Ki=3.72 uM), and SHMT1 (Ki=2.91 uM).
AGF347 did not inhibit MTHFD2 at >200 uM.
AGF347 demonstrated in vitro antitumor efficacies in a pancreatic cancer cell line panel (HPAC IC50=194 nM) and BxPC-3 (IC50=80 nM).
AGF347 targeted SHMT2 in the mitochondria, and SHMT1 and the purine biosynthetic enzymes GARFTase and/or AICARFTase in the cytosol.
AGF347 significant in vivo antitumor efficacy with potential for complete responses against both early-stage and upstage MIA PaCa-2 pancreatic tumor xenografts.

物理化学性质&存储条件

分子量	473.461
分子式	C22H24FN5O6
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	(4-(4-(2-amino-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)butyl)-2-fluorobenzoyl)-l-glutamic acid

参考文献

1. Dekhne AS, et al. Mol Pharmacol. 2020 Jan;97(1):9-22.

2. Dekhne AS, et al. Mol Cancer Ther. 2019 Oct;18(10):1787-1799.

AGF347 (AGF-347)

生物&药学活性

物理化学性质&存储条件

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AGF347 (AGF-347)

生物&药学活性

物理化学性质&存储条件

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