Website:www.dcchemicals.com Email: info@dcchemicals.com Phone:+86-21-58447131 Marketing Center: Room 610,Building 15, Jinxiang Rd 201, Shanghai, China
Datasheet of Chidamide Description:. Chidamide(CS055; HBI-8000) is a class I HDAC inhibitor with IC50s of 95/160/67/733 nM for HDAC1/2/3/8; also inhibits HDAC10/11(IC50=78/432 nM); no inhibition on HDAC4/5/7/9/6(IC50>30 uM). in vitro: Chidamide was able to increase the acetylation levels of histone H3 and to inhibit the PI3K/Akt and MAPK/Ras signaling pathways, which resulted in arresting colon cancer cells at the G1 phase of the cell cycle and promoting apoptosis. chidamide inhibited class I HDACs 1–3, as well as class IIb HDAC10, at low nanomolar concentrations. Chidamide significantly induced histone H3 acetylation in both HeLa human cervical adenocarcinoma cells and human PBMC and the extent of induction was similar to that seen with MS-275 and SAHA. Cell growth inhibition studies performed with 18 human-derived tumor cell lines demonstrated that chidamide and MS-275 similarly inhibited the in vitro growth of most, but not all, tumor cells in the low micromolar concentration range. At low concentrations (<1 μM), CS055 induced G1 arrest. At moderate concentrations (0.5 μM-2 μM), CS055 induced differentiation, as determined by the increased expression of the myeloid differentiation marker CD11b. At relatively high concentrations (2 μM-4 μM), CS055 potently induced caspase-dependent apoptosis. Chidamide treatment significantly decreased the expression of type I HDACs, uncleaved Caspase-3 and p21 and increased the ratio of Bax/Bcl-2 expression. in vivo: chidamide in the dose range of 12.5–50 mg/kg dose-dependently reduced tumor size and tumor weight, and the dose of 50 mg/kg produced similar or greater efficacy compared with the control drugs 5-fluorouracil (5-FU, 20 mg/kg) and MS-275 (25 mg/kg, which was reported as the maximum tolerated dose in xenograft models. Daily oral CS055 treatment of nude mice bearing HL60 cell xenografts suppressed tumour growth, induced tumour cell apoptosis and prolonged the survival of tumour-bearing mice.
Chemical Information Catalog
DC7978
Purity of current batch:
>98%
Molecular Weight (MW)
390.41
Molecular Formula
C22H19FN4O2
CAS No.
743420-02-2
Solubility (25°C)
DMSO
Storage
Store at -20°C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.