天堂网亚洲,天天操天天搞,91视频高清,菠萝蜜视频在线观看入口,美女视频性感美女视频,95丝袜美女视频国产,超高清美女视频图片

ChemicalBook--->CAS DataBase List--->2417012-26-9

2417012-26-9

2417012-26-9 Structure

2417012-26-9 Structure
IdentificationBack Directory
[Name]

1(2H)-Isoquinolinone, 2-[(S)-cyclopropyl(4-methyl-2-pyridinyl)methyl]-5-[1-ethyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-3,4-dihydro-7-(1H-imidazol-1-ylmethyl)-
[CAS]

2417012-26-9
[Synonyms]

WDR5-IN-5
WDR5 inhibitor 41
1(2H)-Isoquinolinone, 2-[(S)-cyclopropyl(4-methyl-2-pyridinyl)methyl]-5-[1-ethyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-3,4-dihydro-7-(1H-imidazol-1-ylmethyl)-
[Molecular Formula]

C29H29F3N6O
[MOL File]

2417012-26-9.mol
[Molecular Weight]

534.58
Chemical PropertiesBack Directory
[Boiling point ]

752.8±60.0 °C(Predicted)
[density ]

1.39±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

6.63±0.12(Predicted)
[color ]

White to light yellow
Hazard InformationBack Directory
[Uses]

WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM[1].
[in vivo]

WDR5-IN-5 (compound 41) (10 mg/kg; p.o.) shows high oral exposure (AUC0,inf=3984 h.ng/mL), long half-life of T1/2=1.3 h[1].
WDR5-IN-5 (3 mg/kg; i.v.) also shows low iv clearance (26 mL/min/kg). WDR5-IN-5 is well tolerated and shows no adverse effects in mice by both i.v. and p.o. dosing[1].
WDR5-IN-5 can be formulated as 0.6 and 1 mg/mL solutions in ethanol, tocopherol poly (ethylene glycol) succinate (TPGS), PEG400 and water (v/v/v/v, 5/5/30/60) for i.v. and p.o. dosing, respectively[1].
PK profile of WDR5-IN-5 in CD-1 Mice[1]

RouteDose (mg/kg)CL (mL/min/kg)AUC0,inf (h.ng/mL)Vss (L/kg)T1/2 (h)F (%)
i.v.32619511.6//
p.o.1020833984/1.361
Animal Model:Male CD-1 mice[1]
Dosage:3 mg/kg i.v.; 10 mg/kg p.o.
Administration:Intravenous injection or oral gavage
Result:Showed high oral exposure (AUC0,inf=3984 h.ng/mL), long half-life of T1/2=1.3 h, and low iv clearance (26 mL/min/kg).
[References]

[1] Teuscher KB, et al. Discovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization. J Med Chem. 2022 Apr 28. 65(8):6287-6312. DOI:10.1021/acs.jmedchem.2c00195
2417012-26-9 suppliers list
Company Name: TargetMol Chemicals Inc.  
Tel: 15002134094
Website: https://www.targetmol.cn/
Tags:2417012-26-9 Related Product Information

  • HomePage | Member Companies | Advertising | Contact us | Previous WebSite | MSDS | CAS Index | CAS DataBase | Privacy | Terms | About Us
  • All products displayed on this website are only for non-medical purposes such as industrial applications or scientific research, and cannot be used for clinical diagnosis or treatment of humans or animals. They are not medicinal or edible.
    According to relevant laws and regulations and the regulations of this website, units or individuals who purchase hazardous materials should obtain valid qualifications and qualification conditions.
  • Copyright © 2023 ChemicalBook All rights reserved.