ChemicalBook >> CAS DataBase List >>4,6-Pyrimidinediamine, 2-[[(1R)-1-[2-[4-methoxy-3-[2-(4-morpholinyl)ethoxy]phenyl]-5-methyl-4-thiazolyl]ethyl]thio]-

4,6-Pyrimidinediamine, 2-[[(1R)-1-[2-[4-methoxy-3-[2-(4-morpholinyl)ethoxy]phenyl]-5-methyl-4-thiazolyl]ethyl]thio]-

4,6-Pyrimidinediamine, 2-[[(1R)-1-[2-[4-methoxy-3-[2-(4-morpholinyl)ethoxy]phenyl]-5-methyl-4-thiazolyl]ethyl]thio]- structure

CAS No.: 2107280-55-5

Chemical Name:: 4,6-Pyrimidinediamine, 2-[[(1R)-1-[2-[4-methoxy-3-[2-(4-morpholinyl)ethoxy]phenyl]-5-methyl-4-thiazolyl]ethyl]thio]-

Synonyms: DI-87;(R)-2-((1-(2-(4-methoxy-3-(2-morpholinoethoxy)phenyl)-5-methylthiazol-4-yl)ethyl)thio)pyrimidine-4,6-diamine;4,6-Pyrimidinediamine, 2-[[(1R)-1-[2-[4-methoxy-3-[2-(4-morpholinyl)ethoxy]phenyl]-5-methyl-4-thiazolyl]ethyl]thio]-

CBNumber:: CB69769379

Molecular Formula:: C23H30N6O3S2

Molecular Weight:: 502.65

MDL Number:

MOL File:: 2107280-55-5.mol

Last updated:2024-07-02 08:55:14

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4,6-Pyrimidinediamine, 2-[[(1R)-1-[2-[4-methoxy-3-[2-(4-morpholinyl)ethoxy]phenyl]-5-methyl-4-thiazolyl]ethyl]thio]- Properties

Boiling point	748.9±70.0 °C(Predicted)
Density	1.37±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
pka	6.39±0.10(Predicted)
form	Solid
color	Off-white to light yellow

4,6-Pyrimidinediamine, 2-[[(1R)-1-[2-[4-methoxy-3-[2-(4-morpholinyl)ethoxy]phenyl]-5-methyl-4-thiazolyl]ethyl]thio]- Chemical Properties,Uses,Production

Biological Activity

DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK[1]. (S)-DI-87 exhibits a much higher IC50 value (IC50=468 nM) relative to DI-87 ((R)-DI-8) (IC50=3.15 nM) in CEM T-ALL cells for inhibition of dCK activity[1]. DI-87 (1 μM; for 72 hours) rescues human cell line CCRF-CEM (CEM) cells from the anti-proliferative effects of gemcitabine, a dCK-dependent nucleoside analog prodrug, with an EC50 of 10.2 nM[1]. DI-87 (5-25 mg/kg; oral gavage) exhibits full dCK inhibition for 27 hours, and enzyme activity fully recovered by 36 hours with 25 mg/kg dose[1]. DI-87 (10-50 mg/kg; oral) has plasma concentrations of between 1 and 3 hours and plasma half-life of 4 hours[1]. DI-87 (10 mg/kg/day or 25 mg/kg/twice a day; oral; for 16-18 days) with thymidine (2 g/kg; ip; twice a day) results in reduced tumor growth in male NSG mice implanted with CEM tumors[1].

References

[1]. Soumya Poddar, et al. Development and Preclinical Pharmacology of a Novel dCK Inhibitor, DI-87. Biochem Pharmacol. 2020 Feb;172:113742.

4,6-Pyrimidinediamine, 2-[[(1R)-1-[2-[4-methoxy-3-[2-(4-morpholinyl)ethoxy]phenyl]-5-methyl-4-thiazolyl]ethyl]thio]- Preparation Products And Raw materials

Raw materials

Preparation Products

4,6-Pyrimidinediamine, 2-[[(1R)-1-[2-[4-methoxy-3-[2-(4-morpholinyl)ethoxy]phenyl]-5-methyl-4-thiazolyl]ethyl]thio]- Suppliers

Global( 3)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
Suzhou Haiben Pharmaceutical Co., Ltd	14760821013 14760821013	1816280386@qq.com	China	6752	58
Soochow Chirally Material Science and Technology Co.,Ltd	0512-66834346 17751187418	szkrl2022@126.com	China	584	58
Shaoyuan Technology (Shanghai) Co., Ltd.	021-50795510 4000665055	sy-c6@accelachem.com	China	10000	58

Supplier	Advantage
Suzhou Haiben Pharmaceutical Co., Ltd	58
Soochow Chirally Material Science and Technology Co.,Ltd	58
Shaoyuan Technology (Shanghai) Co., Ltd.	58

4,6-Pyrimidinediamine, 2-[[(1R)-1-[2-[4-methoxy-3-[2-(4-morpholinyl)ethoxy]phenyl]-5-methyl-4-thiazolyl]ethyl]thio]- DI-87 (R)-2-((1-(2-(4-methoxy-3-(2-morpholinoethoxy)phenyl)-5-methylthiazol-4-yl)ethyl)thio)pyrimidine-4,6-diamine 2107280-55-5