An inhibitor of Hsp90 (IC50 = 0.14 µM); inhibits proliferation of a variety of cancer cell lines

MPC-3100 – 5 mg

Brand:
Cayman
CAS:
958025-66-6
Storage:
-20
UN-No:
Non-Hazardous - /

MPC-3100 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 0.14 µM in a fluorescence polarization assay).{53052} It inhibits proliferation of a variety of cancer cell lines, including colon, prostate, ovarian, gastric, and breast cancer cells (IC50s = 0.2-0.55 µM), as well as MV4-11 leukemia, A549 non-small cell lung cancer (NSCLC), NCI H69 SCLC, and multidrug-resistant NCI/ADR-RES cells (IC50s = 0.25, 0.77, 0.15, and 4.3 µM, respectively). MPC-3100 induces degradation of the Hsp90 client proteins Akt and HER2 (IC50s = 0.1-0.5 µM) and a compensatory Hsp70 response in NCI N87, HCT116, and DU145 cell lysates. It also induces Hsp70 expression in the liver and tumor tissue and reduces tumor growth in an NCI N87 mouse xenograft model when administered at doses of 50 and 75 mg/kg. It induces tumor regression in the same model when administered at doses of 125 and 200 mg/kg.  

 

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Description

An inhibitor of Hsp90 (IC50 = 0.14 µM); inhibits proliferation of a variety of cancer cell lines, including colon, prostate, ovarian, gastric, and breast cancer cells (IC50s = 0.2-0.55 µM), as well as MV4-11 leukemia, A549 NSCLC, NCI H69 SCLC, and multidrug-resistant NCI/ADR-RES cells (IC50s = 0.25, 0.77, 0.15, and 4.3 µM, respectively); induces degradation of Akt and HER2 (IC50s = 0.1-0.5 µM) and a compensatory Hsp70 response in NCI N87, HCT116, and DU145 cell lysates; induces Hsp70 expression in the liver and tumor tissue and reduces tumor growth in an NCI N87 mouse xenograft model at 50 and 75 mg/kg and tumor regression at 125 and 200 mg/kg

Formal name: (2S)-1-[4-[2-[6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)thio]-9H-purin-9-yl]ethyl]-1-piperidinyl]-2-hydroxy-1-propanone

Synonyms: 

Molecular weight: 549.4

CAS: 958025-66-6

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Heat Shock Proteins||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cancer|Multidrug Resistance||Research Area|Cell Biology|Cellular Chaperones

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