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TH-588
CAS No. 1609960-31-7
TH-588( TH588 )
Catalog No. M12322 CAS No. 1609960-31-7
A potent and selective inhibitor of MTH1 protein with IC50 of 5 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 60 | In Stock |
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| 2MG | 33 | In Stock |
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| 5MG | 54 | In Stock |
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| 10MG | 79 | In Stock |
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| 25MG | 122 | In Stock |
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| 50MG | 203 | In Stock |
|
| 100MG | 381 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameTH-588
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NoteResearch use only, not for human use.
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Brief DescriptionA potent and selective inhibitor of MTH1 protein with IC50 of 5 nM.
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DescriptionA potent and selective inhibitor of MTH1 protein with IC50 of 5 nM; shows no relevant inhibition for MTH2,NUDT5, NUDT12,NUDT14,NUDT16 and other proteinswith known nucleoside triphosphate pyrophosphatase activity; causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.
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In VitroCell Viability Assay Cell Line:U2OS, HeLa, MDA-MB-231, MCF-7, SW480, SW620, VH10, HDFn cells Concentration:2, 4, 6, 8, 10 μM Incubation Time:7-10 days Result:Selectively and effectively killed U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC50s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM, but was less toxic to several primary or immortalized cells.
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In VivoAnimal Model:5-6 weeks female SCID mice (SW480 xenograft cancer model)Dosage:30 mg/kg Administration:Subcutaneous injection; once daily for 35 days Result:Reduced tumour growth in SW480 xenograft cancer model.
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SynonymsTH588
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PathwayCell Cycle/DNA Damage
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TargetDNA/RNA Synthesis
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RecptorMTH1
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1609960-31-7
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Formula Weight295.1672
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Molecular FormulaC13H12Cl2N4
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Purity>98% (HPLC)
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SolubilityDMSO: 16 mg/mL
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SMILESNC1=NC(C2=CC=CC(Cl)=C2Cl)=CC(NC3CC3)=N1
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Chemical Name2,4-Pyrimidinediamine, N4-cyclopropyl-6-(2,3-dichlorophenyl)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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DNA polymerase-IN-1
DNA polymerase-IN-1, a DNA polymerase inhibitor, exhibited antiproliferative activity against tumor cells with a half-inhibitory concentration (IC50) of 20.7 μM.
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NSAH?
NSAH is a nonnucleoside inhibitor of human ribonucleotide reductase (hRR).with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively.A unique nonnucleoside small-molecule hRR inhibitor, naphthyl salicylic acyl hydrazone (NSAH), using virtual screening, binding affinity, inhibition, and cell toxicity assays.?NSAH binds to hRRM1 with an apparent dissociation constant of 37 μM, and steady-state kinetics reveal a competitive mode of inhibition.?
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Mefenidil
Mefenidil (McN-2378), a selective cerebral vasodilator, was shown to increase CBF in healthy brains without stimulating O2 uptake in a dog anesthesia model.
