TH 9619 disodium salt

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Description: MTHFD2 inhibitor
Chemical Name: Disodium N-[[5-[[2-(2,4-Diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)acetyl]amino]-3-fluoro-2-pyridinyl]carbonyl]-L-glutamate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for TH 9619 disodium salt

TH 9619 disodium salt is a potent and selective methylenetetrahydrofolate dehydrogenase inhibitor (MTHFD2; IC50 = 47 nM). It shows efficacity on HL-60 cell viability with EC50 of 11nM. In vitro, It shows antiproliferative efficacy in acute myeloid leukemia (AML) cells and T-ALL Jurkat cells. In vivo, TH9619 disodium salt impairs cancer progression in a mouse disease model of AML.

Licensing Information

Sold under license from Thomas Helleday's Foundation for Medical Research and One-Carbon Therapeutics

Technical Data for TH 9619 disodium salt

M. Wt 495.33
Formula C17H16FN7Na2O7
Storage Store at -20°C
Purity ≥98% (HPLC)
InChI Key AKIUEXPYEGJOLL-WWPIYYJJSA-L
Smiles NC1=NC(C(CC(NC2=CN=C(C(F)=C2)C(N[C@H](C(O[Na])=O)CCC(O[Na])=O)=O)=O)=C(N1)N)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for TH 9619 disodium salt

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 9.91 20 with gentle warming

Preparing Stock Solutions for TH 9619 disodium salt

The following data is based on the product molecular weight 495.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 10.09 mL 50.47 mL 100.94 mL
1 mM 2.02 mL 10.09 mL 20.19 mL
2 mM 1.01 mL 5.05 mL 10.09 mL
10 mM 0.2 mL 1.01 mL 2.02 mL

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Product Datasheets for TH 9619 disodium salt

References for TH 9619 disodium salt

References are publications that support the biological activity of the product.

Bonagas et al (2022) Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress. Nat.Cancer 3 156 PMID: 35228749


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Citations for TH 9619 disodium salt

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Literature in this Area

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