TH287
Synonym(s):6-(2,3-Dichlorophenyl)-N4-methylpyrimidine-2,4-diamine hydrochloride
- CAS NO.:1609960-30-6
- Empirical Formula: C11H10Cl2N4
- Molecular Weight: 269.13
- MDL number: MFCD29035111
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-08 09:02:24
What is TH287?
Description
Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH287 is an MTH1 inhibitor (IC50 = 0.8 nM) that selectively kills cancer cell lines (IC50s = 0.8-3.06 μM) without significant cytotoxicity towards primary or immortalized cells (IC50s = ≥20 μM). At up to 100 μM it does not show significant effect towards the related nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, as well as other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase, and ITPA).
The Uses of TH287
6-(2,3-Dichlorophenyl)-N4-methyl-2,4-pyrimidinediamine is known to possess antitumor effects and nanomolar MTH1-inhibitory activity in vitro for cancer cell survival.
References
1. gad h, koolmeister t, jemth as et al. mth1 inhibition eradicates cancer by preventing sanitation of the dntp pool. nature. 2014 apr 10;508(7495):215-21.
Properties of TH287
Boiling point: | 512.2±60.0 °C(Predicted) |
Density | 1.440±0.06 g/cm3(Predicted) |
storage temp. | 2-8°C |
solubility | DMSO: soluble5mg/mL, clear (warmed) |
pka | 5.91±0.10(Predicted) |
form | powder |
color | white to beige |
Safety information for TH287
Signal word | Danger |
Pictogram(s) |
Corrosion Corrosives GHS05 Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H318:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. |
Computed Descriptors for TH287
New Products
6-Bromo 2-Iodo Indole Pyridine 2,4,6-Tricarboxaldehyde Fosfomycin EP impurity D Rimegepant Impurity 3 Ivermectin EP Impurity B Tubulysin E Tubulysin A (2S,4R)-4-amino-2-methyl-5-phenylpentanoic acid hydrochloride Tubulysin F Calcium Sodium Phosphosilicate IH 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate Fuel shell (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol 3,3,6,6-Tetramethylcyclohexane-1,2-dione 3-Morpholino-5,6-dihydropyridin-2(1H)-one 2-Ethoxy-4-nitrobenzoic acid (1-Isopropyl-1H-pyrazol-5-yl)boronic acid 2-Chloro-3-(chloromethyl)pyridine 3,6-Bis(4-iodophenyl)-2,5-dihydropyrrolo[3,4-c]pyrrole-1,4-dione 1,3,5-Trimethyl-1,4-cyclohexadiene 6-bromopyridazin-3-amine Ethyl (2Z)-chloro((4-methoxyphenyl)hydrazono)acetateRelated products of tetrahydrofuran
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