DGY-06-116
- Product Name
- DGY-06-116
- CAS No.
- 2556836-50-9
- Chemical Name
- DGY-06-116
- Synonyms
- DGY-06-116;DGY-06-116 ,S9643;DGY06116,DGY 06 116;4-((2-Acrylamidophenyl)amino)-N-(2-chloro-6-methylphenyl)-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide;5-Pyrimidinecarboxamide, N-(2-chloro-6-methylphenyl)-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-[[2-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-
- CBNumber
- CB28077938
- Molecular Formula
- C32H33ClN8O2
- Formula Weight
- 597.11
- MOL File
- 2556836-50-9.mol
DGY-06-116 Property
- Density
- 1.347±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 250 mg/mL (418.68 mM; Need ultrasonic)
- form
- Solid
- pka
- 10.42±0.70(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 025863
- Product name
- DGY-06-116
- Packaging
- 001
- Price
- $600
- Updated
- 2021/12/16
- Product number
- 025863
- Product name
- DGY-06-116
- Packaging
- 002
- Price
- $1100
- Updated
- 2021/12/16
- Product number
- 025863
- Product name
- DGY-06-116
- Packaging
- 003
- Price
- $2100
- Updated
- 2021/12/16
DGY-06-116 Chemical Properties,Usage,Production
Uses
DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC50 of 3nM. DGY-06-116 inhibits FGFR1 with an IC50 of 8340 nM[1].
in vivo
DGY-06-116 (Compound 15a; 5 mg/kg for 3 times every 12 h via intraperitoneal injection) is able to inhibit SRC for an extended duration in adult C57B6 mice, likely due to its ability to covalently bind the target[1].
DGY-06-116 exhibits a short half-life and high exposure (T1/2=1.29 h, AUC=12 746.25 min·ng/mL) following i.p. administration (5 mg/kg) in B6 mice[1].
| Animal Model: | Adult C57B6 mice[1] |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection; for 3 times every 12 h |
| Result: | Led to inhibition of p-SRCY416 at 2 and 4 h postdosing, compared to the vehicle controls. Demonstrated SRC binding and inhibition at both 2 and 4 h postdosing compared to the vehicle controls. |
References
[1] Guangyan Du, et al. Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine. J Med Chem. 2020 Feb 27;63(4):1624-1641. DOI:10.1021/acs.jmedchem.9b01502
[2] Deepak Gurbani, et al. Structure and Characterization of a Covalent Inhibitor of Src Kinase. Front Mol Biosci. 2020 May 19;7:81. DOI:10.3389/fmolb.2020.00081
DGY-06-116 Preparation Products And Raw materials
Raw materials
Preparation Products
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