TH287 is , while it's Molecular Formula is C11H10Cl2N4. 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.

What is the CAS number for TH287?

The CAS number of TH287 is 1609960-30-6.

What is TH287 (1609960-30-6) used for?

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).

TH287 is , while it's Molecular Formula is C11H10Cl2N4. 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.

What is the CAS number for TH287?

The CAS number of TH287 is 1609960-30-6.

What is TH287 (1609960-30-6) used for?

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).

Product classification

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1609960-30-6

Product Name:TH287
Molecular Formula:C12H11Cl2N3
Molecular Weight:269.133

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Product Details

Purity:99%

Manufacturer Sells Best Quality TH287 1609960-30-6 with stock

Molecular Formula:C11H10Cl2N4
Molecular Weight:269.133
Boiling Point:512.2±60.0 °C(Predicted)
PKA:5.91±0.10(Predicted)
PSA：37.81000
Density:1.440±0.06 g/cm3(Predicted)
LogP:3.87350

1609960-30-6 Relevant articles

Method for synthesizing MTH1 protein inhibitors TH287

-

Paragraph 0017; 0019, (2016/10/10)

The invention discloses a method for syn...

MTH1 INHIBITORS FOR TREATMENT OF INFLAMMATORY AND AUTOIMMUNE CONDITIONS

-

Page/Page column 91; 105; 106, (2016/04/04)

A compound of formula (I), or a pharmace...

PYRIMIDINE-2,4-DIAMINE DERIVATIVES FOR TREATMENT OF CANCER

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Page/Page column 97; 108, (2014/06/23)

A compound of formula (I), or a pharmace...

1609960-30-6 Process route

: 1604677-77-1
4-chloro-6-(2,3-dichlorophenyl)pyrimidin-2-amine

: 74-89-5
methylamine

: 1609960-30-6
6-(2,3-dichlorophenyl)-4-N-methylpyrimidine-2,4-diamine

Conditions

Conditions	Yield
With N-ethyl-N,N-diisopropylamine; In butan-1-ol; at 95 ℃;
With N-ethyl-N,N-diisopropylamine; In butan-1-ol; at 95 ℃;

: 1005-37-4
2-amino-4-methylamino-6-chloropyrimidine

: 151169-74-3
2,3-dichlorobenzeneboronic acid

: 1609960-30-6
6-(2,3-dichlorophenyl)-4-N-methylpyrimidine-2,4-diamine

Conditions

Conditions	Yield
2-amino-4-methylamino-6-chloropyrimidine; 2,3-dichlorobenzeneboronic acid; With sodium carbonate; In 1,2-dimethoxyethane; water; for 0.5h; Inert atmosphere; With tetrakis(triphenylphosphine) palladium⁽⁰⁾; In 1,2-dimethoxyethane; at 90 ℃; for 48h; Inert atmosphere;

1609960-30-6 Upstream products

1604677-77-1
4-chloro-6-(2,3-dichlorophenyl)pyrimidin-2-amine
74-89-5
methylamine
151169-74-3
2,3-dichlorobenzeneboronic acid
1005-37-4
2-amino-4-methylamino-6-chloropyrimidine

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