DC Chemicals supplies: CUDC-101,cas: 1012054-59-9,Catalog: DC7544,In stock.
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Product name: CUDC-101, Synonyms: CUDC101,CUDC 101, cas: 1012054-59-9, MW: 434.49, Molecule Formula: C24H26N4O4
CUDC-101, cas 1012054-59-9, Purity>98%. Best price and quality from DC Chemicals. Bromosporine is a broad spectrum bromodomain inhibitor. Accelerates FRAP recovery of BRD4 and CREBBP in cells at a concentration of 1 μM.
Specific For class I and class II HDACs, CUDC-101 does not inhibit class III Sir-type HDACs. CUDC-101 displays weak activity against other protein kinases including KDR/VEGFR2, Lyn, Lck, Abl-1, FGFR-2, Flt-3, and Ret with IC50 of 0.85 μM, 0.84 μM, 5.91 μM, 2.89 μM, 3.43 μM, 1.5 μM, abd 3.2 μM, respectively. CUDC-101 displays broad antiproliferative activity in many human cancer cell types with IC50 of 0.04-0.80 μM, exhibiting a higher potency than erlotinib, lapatinib, and combinations of vorinostat with either erlotinib or lapatinib in most cases. CUDC-101 potently inhibits lapatinib- and erlotinib-resistant cancer cell lines.CUDC-101 inhibits the erlotinib-resistant EGFR mutant T790M although its effects are incomplete with an Amax of ~60% of peak enzyme activity after inhibition. CUDC-101 treatment increases the acetylation of histone H3 and H4, as well as the acetylation of non-histone substrates of HDAC such as p53 and α-tubulin, in a dose-dependant manner in various cancer cell lines. CUDC-101 also suppresses HER3 expression, Met amplification, and AKT reactivation in tumor cells. Administration of CUDC-101 at 120 mg/kg/day induces tumor regression in the Hep-G2 liver cancer model, which is more efficacious than that of erlotinib at its maximum tolerated dose (25 mg/kg/day) and vorinostat at an equimolar concentration dose (72 mg/kg/day). CUDC-101 inhibits the growth of erlotinib-sensitive H358 NSCLC xenografts in a dose-dependent manner. CUDC-101 also shows potent inhibition of tumor growth in the erlotinib-resistant A549 NSCLC xenograft model. CUDC-101 produces significant tumor regression in the lapatinib-resistant, HER2-negative, EGFR-overexpressing MDA-MB-468 breast cancer model and the EGFR-overexpressing CAL-27 head and neck squamous cell carcinoma (HNSCC) model. Additionally, CUDC-101 inhibits tumor growth in the K-ras mutant HCT116 colorectal and EGFR/HER2 (neu)-expressing HPAC pancreatic cancer models. [1]For the detailed information of CUDC-101, the solubility of CUDC-101 in water, the solubility of CUDC-101 in DMSO, the solubility of CUDC-101 in PBS buffer, the animal experiment (test) of CUDC-101, the cell expriment (test) of CUDC-101, the in vivo, in vitro and clinical trial test of CUDC-101, the EC50, IC50,and Affinity of CUDC-101, Please contact DC Chemicals.
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