Glycine, N-[4-[[2-(1-pyrrolidinyl)-4-pyrimidinyl]amino]phenyl]-N-[(2,4,6-trimethylphenyl)sulfonyl]-
- Product Name
- Glycine, N-[4-[[2-(1-pyrrolidinyl)-4-pyrimidinyl]amino]phenyl]-N-[(2,4,6-trimethylphenyl)sulfonyl]-
- CAS No.
- 2355377-13-6
- Chemical Name
- Glycine, N-[4-[[2-(1-pyrrolidinyl)-4-pyrimidinyl]amino]phenyl]-N-[(2,4,6-trimethylphenyl)sulfonyl]-
- Synonyms
- DDO-5936;DDO-5936, 10 mM in DMSO;N-(Mesitylsulfonyl)-N-(4-((2-(pyrrolidin-1-yl)pyrimidin-4-yl)amino)phenyl)glycine;Glycine, N-[4-[[2-(1-pyrrolidinyl)-4-pyrimidinyl]amino]phenyl]-N-[(2,4,6-trimethylphenyl)sulfonyl]-;Inhibitor,DDO-5936,DDO 5936,colorectal,specific,inhibit,Glu47,potent,DDO5936,HSP,Heat shock proteins,Hsp90,cancer
- CBNumber
- CB88800341
- Molecular Formula
- C25H29N5O4S
- Formula Weight
- 495.59
- MOL File
- 2355377-13-6.mol
Glycine, N-[4-[[2-(1-pyrrolidinyl)-4-pyrimidinyl]amino]phenyl]-N-[(2,4,6-trimethylphenyl)sulfonyl]- Property
- Boiling point:
- 752.5±70.0 °C(Predicted)
- Density
- 1.361±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Acetonitrile: Slightly Soluble: 0.1-1 mg/ml
Chloroform: Slightly Soluble: 0.1-1 mg/ml
DMSO: Sparingly Soluble: 1-10 mg/ml - form
- Solid
- pka
- 3.12±0.10(Predicted)
- color
- White to yellow
Glycine, N-[4-[[2-(1-pyrrolidinyl)-4-pyrimidinyl]amino]phenyl]-N-[(2,4,6-trimethylphenyl)sulfonyl]- Chemical Properties,Usage,Production
Uses
DDO-5936 is a potent and specific Hsp90-Cdc37 PPI inhibitor. DDO-5936 can be used for the research of colorectal cancer[1].
Biological Activity
DDO-5936 is a potent and specific Hsp90-Cdc37 PPI inhibitor. DDO-5936 can be used for the research of colorectal cancer[1]. DDO-5936 is a Hsp90-Cdc37 PPI inhibitor with potency and specificity through binding to a critical site on Hsp90 involving Glu47[1]. DDO-5936 (0~80 mg/kg; p.o.) shows effect at the high dose group[1].DDO-5936 is well tolerated for the absence of serious weight loss. DDO-5936 high dose groups show that tumor cells in the xenografts decreased significantly. DDO-5936 shows limited oral efficiency[1].
in vivo
DDO-5936 (0~80 mg/kg; p.o.) shows effect at the high dose group[1].
DDO-5936 is well tolerated for the absence of serious weight loss. DDO-5936 high dose groups show that tumor cells in the xenografts decreased significantly. DDO-5936 shows limited oral efficiency[1].
| Animal Model: | Mice[1] |
| Dosage: | 0~80 mg/kg |
| Administration: | P.o. |
| Result: | Showed a moderate effect at the high dose group. |
References
[1] Wang L, et al. Discovery and Optimization of Small Molecules Targeting the Protein-Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer. J Med Chem. 2020;63(3):1281-1297.
[2] LEI WANG. Small-molecule inhibitor targeting the Hsp90-Cdc37 protein-protein interaction in colorectal cancer[J]. Science Advances, 2019, 5 9. DOI: 10.1126/sciadv.aax2277
Glycine, N-[4-[[2-(1-pyrrolidinyl)-4-pyrimidinyl]amino]phenyl]-N-[(2,4,6-trimethylphenyl)sulfonyl]- Preparation Products And Raw materials
Raw materials
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