WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130558
CAS#: 2379556-22-4 (free acid)
Description: TH9619 is a potent inhibitor of dehydrogenase and cyclohydrolase activities in both MTHFD1 and MTHFD2, and selectively kills cancer cells. TH9619 targets nuclear MTHFD2 but does not inhibit mitochondrial MTHFD2. TH9619 inhibits the activity of MTHFD1 occurring downstream of mitochondrial formate release, leading to the accumulation of 10-formyl-tetrahydrofolate.
Hodoodo Cat#: H130558
Name: TH9619
CAS#: 2379556-22-4 (free acid)
Chemical Formula: C17H18FN7O7
Exact Mass: 451.13
Molecular Weight: 451.370
Elemental Analysis: C, 45.24; H, 4.02; F, 4.21; N, 21.72; O, 24.81
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Related CAS #: 2379556-22-4 (free acid) TH9619 disodium
Synonym: TH 9619, TH-9619
IUPAC/Chemical Name: (5-(3-(4,6-Diamino-2-oxo-1,2-dihydropyridin-3-yl)ureido)-3-fluoropicolinoyl)-L-glutamic acid
InChi Key: UOXSYJABLLZCDI-VIFPVBQESA-N
InChi Code: InChI=1S/C17H18FN7O7/c18-7-3-6(22-17(32)25-13-8(19)4-10(20)24-15(13)29)5-21-12(7)14(28)23-9(16(30)31)1-2-11(26)27/h3-5,9H,1-2H2,(H,23,28)(H,26,27)(H,30,31)(H2,22,25,32)(H5,19,20,24,29)/t9-/m0/s1
SMILES Code: O=C(O)CC[C@@H](C(O)=O)NC(C1=NC=C(NC(NC2=C(N)C=C(N)NC2=O)=O)C=C1F)=O
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Cancer cells fuel their increased need for nucleotide supply by upregulating one-carbon (1C) metabolism, including the enzymes methylenetetrahydrofolate dehydrogenase-cyclohydrolase 1 and 2 (MTHFD1 and MTHFD2).
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 451.37 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.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1. Green AC, Marttila P, Kiweler N, Chalkiadaki C, Wiita E, Cookson V, Lesur A, Eiden K, Bernardin F, Vallin KSA, Borhade S, Long M, Ghahe EK, Jiménez-Alonso JJ, Jemth AS, Loseva O, Mortusewicz O, Meyers M, Viry E, Johansson AI, Hodek O, Homan E, Bonagas N, Ramos L, Sandberg L, Frödin M, Moussay E, Slipicevic A, Letellier E, Paggetti J, Sørensen CS, Helleday T, Henriksson M, Meiser J. Formate overflow drives toxic folate trapping in MTHFD1 inhibited cancer cells. Nat Metab. 2023 Apr;5(4):642-659. doi: 10.1038/s42255-023-00771-5. Epub 2023 Apr 3. PMID: 37012496; PMCID: PMC10132981.
2. Bonagas, N., Gustafsson, N.M.S., Henriksson, M. et al. Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress. Nat Cancer 3, 156–172 (2022). https://doi.org/10.1038/s43018-022-00331-y