TH588
- Product Name
- TH588
- CAS No.
- 1609960-31-7
- Chemical Name
- TH588
- Synonyms
- TH588;CS-1701;TH588, >98%;TH588(TH-588);TH 588;TH-588;TH588;N4-cyclopropyl-6-(2,3-dic;6-(2,3-dichlorophenyl)-N4-cyclopropylpyrimidine-2,4-diamine;N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine;N4-Cyclopropyl-6-(2,3-dichlorophenyl)-2,4-pyrimidinediamine;2,4-Pyrimidinediamine, N4-cyclopropyl-6-(2,3-dichlorophenyl)-
- CBNumber
- CB02741567
- Molecular Formula
- C13H12Cl2N4
- Formula Weight
- 295.17
- MOL File
- 1609960-31-7.mol
TH588 Property
- Boiling point:
- 545.7±60.0 °C(Predicted)
- Density
- 1.505±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO (up to 5 mg/ml).
- form
- powder
- pka
- 5.90±0.10(Predicted)
- color
- white to light brown
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Safety
- WGK Germany
- 3
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML1096
- Product name
- TH588 hydrochloride
- Purity
- ≥98%(HPLC)
- Packaging
- 5mg
- Price
- $166
- Updated
- 2024/03/01
- Product number
- SML1096
- Product name
- TH588 hydrochloride
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $631
- Updated
- 2024/03/01
- Product number
- 18133
- Product name
- TH588
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 18133
- Product name
- TH588
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2024/03/01
- Product number
- 18133
- Product name
- TH588
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $153
- Updated
- 2024/03/01
TH588 Chemical Properties,Usage,Production
Description
TH588 (1609960-31-7) is a first-in-class nudix hydrolase family inhibitor.1?MTH1/NUDT1 is a family member that “sanitizes” oxidized deoxynucleotide triphosphates (dNTP) preventing their incorporation into DNA and thus avoiding DNA damage and cell death.? TH588 inhibits MTH1/NUDT1 (IC50?= 5 nM) leading to cell death in several cancer cell lines while not affecting normal cells.? Active?in vitro?and?in vivo.? Recent evidence has raised doubts about the cancer-killing ability of MTH1 inhibition.2,3?Conversely, TH588 has been also shown to decrease osteosarcoma cell viability, impair cell cycle, and increase apoptosis via an MTH1-dependent pathway.4
Uses
TH 588 acts as a novel potent and selective permeable inhibitor of the nudix hydrolase MTH1 protein. It acts as a good tool to show the non-oncogene addiction concept to anti-cancer treatments.
Biochem/physiol Actions
TH588 is a potent inhibitor of human 7,8-Dihydro-8-oxoguaninetriphosphatase MTH1 (NUDT1) with an IC50 value of 5 nM and good metabolic stability. MTH1 hydrolyzes oxidized purine nucleoside triphosphates that might otherwise be incorporated into DNA/RNA and contribute to DNA damage. MTH1 removal of oxidized nucleotides that result from increased levels of reactive oxygen species (ROS) in fast-proliferating cancer cells helps protect cancer cells from proliferative stress and prevent cancer cell death. TH588 is considered a new target for cancer therapy. TH588 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family or a panel of 87 enzymes, GPCRs, kinases, ion channels and transporter. TH588 has been shown to selectively kill a variety of cancer cell lines and with in vivo activity shown for TH588 in SW480 colorectal and MCF7 breast tumour xenografts.
storage
Store at -20°C
References
1) Gad?et al. (2014),?MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool; Nature,?508?215 2) Petrocchi et al. (2016)?Identification of potent and selective MTH1 inhibitors; Bioorg. Med. Chem. Lett.,?26?1503 3) Kettle?et al. (2016),?Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival; J. Med. Chem.,?59?2346 4) Moukengue?et al. (2020),?TH1579, MTH1 inhibitor, delays tumour growth and inhibits metastases development in osteosarcoma model; EBioMedicine,?53?102704
TH588 Preparation Products And Raw materials
Raw materials
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View Lastest Price from TH588 manufacturers
- Product
- N4-Cyclopropyl-6-(2,3-dichlorophenyl)-2,4-pyrimidinediamine;TH588;N4-cyclopropyl-6-(2,3-dic 1609960-31-7
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 95%~99%
- Supply Ability
- per week 100kg
- Release date
- 2019-09-05