1H-Indole-3-carbonitrile, 2-amino-6-[2-(3-fluorophenyl)ethenyl]-
- Product Name
- 1H-Indole-3-carbonitrile, 2-amino-6-[2-(3-fluorophenyl)ethenyl]-
- CAS No.
- 2449301-27-1
- Chemical Name
- 1H-Indole-3-carbonitrile, 2-amino-6-[2-(3-fluorophenyl)ethenyl]-
- Synonyms
- CID 137319705;GSK-2643943A,GSK2643943A;GSK2643943A, 10 mM in DMSO;2-amino-6-(3-fluorostyryl)-1H-indole-3-carbonitrile;1H-Indole-3-carbonitrile, 2-amino-6-[2-(3-fluorophenyl)ethenyl]-
- CBNumber
- CB08118811
- Molecular Formula
- C17H12FN3
- Formula Weight
- 277.3
- MOL File
- 2449301-27-1.mol
1H-Indole-3-carbonitrile, 2-amino-6-[2-(3-fluorophenyl)ethenyl]- Property
- Boiling point:
- 540.4±50.0 °C(Predicted)
- Density
- 1.33±0.1 g/cm3(Predicted)
- solubility
- DMSO:90.0(Max Conc. mg/mL);324.56(Max Conc. mM)
Ethanol:8.0(Max Conc. mg/mL);28.85(Max Conc. mM) - pka
- 16.49±0.30(Predicted)
- form
- Solid
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- CS-0041056
- Product name
- GSK2643943A
- Purity
- 98.31%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- CS-0041056
- Product name
- GSK2643943A
- Purity
- 98.31%
- Packaging
- 10mg
- Price
- $165
- Updated
- 2021/12/16
- Product number
- CS-0041056
- Product name
- GSK2643943A
- Purity
- 98.31%
- Packaging
- 25mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0041056
- Product name
- GSK2643943A
- Purity
- 98.31%
- Packaging
- 50mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0041056
- Product name
- GSK2643943A
- Purity
- 98.31%
- Packaging
- 100mg
- Price
- $950
- Updated
- 2021/12/16
1H-Indole-3-carbonitrile, 2-amino-6-[2-(3-fluorophenyl)ethenyl]- Chemical Properties,Usage,Production
Uses
GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) [1][2].
in vivo
GSK2643943A (5 mg/kg, i.p., daily, for 6 days) potentiates oHSV-1-induced oncolysis in SCC9 tumors[2].
?
GSK2643943A (2.5 mg/kg, i.p., daily, for 9 days) plays a regulatory role in oHSV-1 T1012G replication and oncolysis in SCC7 cells[2].
| Animal Model: | The subcutaneous xenograft model[2]. (SCC9 or SCC7 cells (8×106 cells or 1×106 cells), 5-week-old, female, BALB/c nude mice or C3H/HeN mice, four groups, n = 6-7, per group)[2] |
| Dosage: | 5 mg/kg |
| Administration: | GSK2643943A (alone): intraperitoneal administration, daily, for 6 days. GSK2643943A (combination): intraperitoneal administration, daily for 6 days + intratumoral injection with 50 mL of 1×106 PFU T1012G in PBS on day 1, day 4, and day 7. |
| Result: | Caused a visible drop of tumor volumes and significantly reduced the tumor volumes in mice with combined treatment of GSK2643943A and oHSV-1 T1012G. Increased slightly viral ICP0 and gD mRNA accumulation in SCC9 tumors. |
| Animal Model: | The SCC7 mouse model[2]. |
| Dosage: | 2.5 mg/kg |
| Administration: | GSK2643943A (alone): intraperitoneal administration, daily, for 9 days. GSK2643943A (combination): intraperitoneal administration, daily, for 9 days + intratumoral injection, with 50 mL of 1×107 PFU T1012G in PBS on days 1, 4, 7, and 10. |
| Result: | Caused a visible drop of tumor volumes, significantly reduced in mice with combined treatment of GSK and oHSV-1 T1012G. Increased slightly viral ICP0 and gD mRNA accumulation in SCC7 tumors. |
References
[1] Nishi Kumari, et al. Targeting the Ubiquitin Proteasome System in Cancer. Shahzad, Hafiz Naveed (2018). Neoplasm Targeting the Ubiquitin Proteasome System in Cancer. , 10.5772/intechopen.69560(Chapter 8).
[2] Ruitao Lu, et al. USP18 and USP20 restrict oHSV-1 replication in resistant human oral squamous carcinoma cell line SCC9 and affect the viability of SCC9 cells. Mol Ther Oncolytics. 2021 Nov 11;23:477-487. DOI:10.1016/j.omto.2021.11.004
1H-Indole-3-carbonitrile, 2-amino-6-[2-(3-fluorophenyl)ethenyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
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