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ChemicalBook >> CAS DataBase List >>2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)-

2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)-

2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)- Structure
2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)- structure
CAS No.
2259641-46-6
Chemical Name:
2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)-
Synonyms
DS-9300;2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)-
CBNumber:
CB212730052
Molecular Formula:
C25H26F3N5O3
Molecular Weight:
501.5
MDL Number:
MOL File:
2259641-46-6.mol
Last updated:2025-04-18 09:51:51
Request For Quotation

2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)- Properties

Boiling point 759.5±60.0 °C(Predicted)
Density 1.42±0.1 g/cm3(Predicted)
pka 10.48±0.40(Predicted)
form Solid
color White to off-white

2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)- Chemical Properties,Uses,Production

Uses

DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research[1].

in vivo

DS-9300 (p.o., 0.3-3 mg/kg, once daily, 33days) shows dose-dependent antitumor activity with 39%, 74% and 109% tumor growth inhibition at 0.3, 1 and 3 mg/kg, respectively, and no significant toxic effects in Castrated VCaP xenograft mouse model[1].
The pharmacokinetic parameters of DS-9300 in BALB/c mice

PO(10 mg/kg)IV(1 mg/kg)
AUC, AUCu (μM*h)Cmax (μM)T1/2 (h)<Vdss (L/kg)CL, CLu (mL/min/kg)F%
130, 5.33342.40.141.6, 3962

References

[1] Ryutaro Kanada, et al. Discovery of DS-9300: A Highly Potent, Selective, and Once-Daily Oral EP300/CBP Histone Acetyltransferase Inhibitor. J Med Chem. 2023 Jan 12;66(1):695-715. DOI:10.1021/acs.jmedchem.2c01641

2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)- Preparation Products And Raw materials

Raw materials

Preparation Products

2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)- Suppliers

Global( 5)Suppliers
Supplier Tel Email Country ProdList Advantage
Shanghai Chaolan Chemical Technology Center 021-QQ：65489617 15618227136 Sales@ATKchemical.com China 9848 58
TargetMol Chemicals Inc. 4008200310 marketing@tsbiochem.com China 24989 58
SuZhou GoodChemTech Co., Ltd 18136139868; 18136139868 jinlun@goodchemtech.cn China 273 58
Anhui JYHX CO., LTD. 0551-68788198 13295518198 wangyanan@ahjyhx.com China 1759 58
Nanjing Shizhou Biology Technology Co.,Ltd 025-85560043 15850508050 cindy.huang@synzest.com China 12000 58
Supplier Advantage
Shanghai Chaolan Chemical Technology Center 58
TargetMol Chemicals Inc. 58
SuZhou GoodChemTech Co., Ltd 58
Anhui JYHX CO., LTD. 58
Nanjing Shizhou Biology Technology Co.,Ltd 58
2-Pyrrolidinecarboxamide, 1-[[4,4-difluoro-1-(4-methoxyphenyl)cyclohexyl]carbonyl]-4-fluoro-N-1H-pyrazolo[4,3-b]pyridin-5-yl-, (2R,4R)- DS-9300 2259641-46-6