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产品名称 TH 588 hydrochloride
产品货号 Axon 2272 CAS [N.A.] MF C13H12ClN4.HClMW 331.63 Purity: 99% Soluble in DMSO Description First-in-class MTH1 inhibitor (IC50 value 5.0 nM) that selectively and effectively kills U2OS and other cancer cell lines, with considerably less toxicity towards several primary or immortalized cells. Similar to TH 287, TH 588 shows no relevant inhibitory effect for any of the other tested nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, nor for other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase and ITPA).Replacement of the methyl group by a cyclopropyl substituent in TH 588 (compared to TH 287, Axon 2271) improved metabolic stability both in vitro and in vivo, while maintaining MTH1 potency. References Certificates Categories Extra info H. Gad et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature 2014, 508, 215-221.   Y. Nakabeppu et al. MTH1, an oxidized purine nucleoside triphosphatase, prevents the cytotoxicity and neurotoxicity of oxidized purine nucleotides. DNA Repair 2006, 5, 761-772. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology DNA-damage Response MTH1 EC 3.6.1.56 First-in-class MTH1 inhibitor Chemical name N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine hydrochloride Parent CAS No. [1609960-31-7] Order Size Unit Price Stock 5 mg €90.00 In Stock
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TH 588 hydrochloride

Based on 14 reference(s) in Google Scholar 8 10 14

Axon 2272

CAS [N.A.]

MF C13H12ClN4.HCl
MW 331.63

  • Purity: 99%
  • Soluble in DMSO

TH 588 hydrochloride

Description

First-in-class MTH1 inhibitor (IC50 value 5.0 nM) that selectively and effectively kills U2OS and other cancer cell lines, with considerably less toxicity towards several primary or immortalized cells. Similar to TH 287, TH 588 shows no relevant inhibitory effect for any of the other tested nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, nor for other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase and ITPA).
Replacement of the methyl group by a cyclopropyl substituent in TH 588 (compared to TH 287, Axon 2271) improved metabolic stability both in vitro and in vivo, while maintaining MTH1 potency.
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