[CAS NO. 910462-43-0] Domatinostat (4SC-202)
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PRODUCTS SPECIFICATIONS [910462-43-0]
Store
Catalog
SLK-S7555
Brand
Selleck
CAS
910462-43-0
DESCRIPTION [910462-43-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 447.51 |
| Molecular Formula | C23H21N5O3S |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2346 mL | 11.1729 mL | 22.3459 mL |
| 5 mM | 0.4469 mL | 2.2346 mL | 4.4692 mL |
| 10 mM | 0.2235 mL | 1.1173 mL | 2.2346 mL |
| 50 mM | 0.0447 mL | 0.2235 mL | 0.4469 mL |
Description
Domatinostat (4SC-202) is a selective class I inhibitor with of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against . Phase 1.
Targets
In vitro
In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM.
In vivo
In vivo, 4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model.
References
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