| Identification | Back Directory | [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)- | [CAS]
2259641-46-6 | [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)- | [Molecular Formula]
C25H26F3N5O3 | [MOL File]
2259641-46-6.mol | [Molecular Weight]
501.5 |
| Chemical Properties | Back Directory | [Boiling point ]
759.5±60.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
10.48±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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, 5.33 | 34 | 2.4 | 0.14 | 1.6, 39 | 62 | |
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| [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 |
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