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CCT018159 is a 3,4-diarylpyrazole resorcinol, an ATP-competitive HSP90ATPase inhibitor that inhibits human Hsp90β and yeast Hsp90 with IC50s of 3.2 and 6.6 μM, respectively.CCT018159 inhibits key endothelial and tumor cell functions associated with invasion and angiogenesis. CCT018159 caused cellular inhibition associated with G1 phase block and induced apoptosis.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $113 | In Stock | |
25 mg | $227 | In Stock | |
50 mg | $343 | In Stock | |
100 mg | $497 | In Stock |
Description | CCT018159 is a 3,4-diarylpyrazole resorcinol, an ATP-competitive HSP90ATPase inhibitor that inhibits human Hsp90β and yeast Hsp90 with IC50s of 3.2 and 6.6 μM, respectively.CCT018159 inhibits key endothelial and tumor cell functions associated with invasion and angiogenesis. CCT018159 caused cellular inhibition associated with G1 phase block and induced apoptosis. |
Targets&IC50 | HSP90:3.2 µM, HSP90 (yeast):6.6 μM, HSP90 β (human):3.2 μM |
In vitro | CCT018159 (100 nM-10 μM) decreased POMC mRNA levels in AtT-20 cells and ACTH levels in the culture medium of these cells, suggesting that CCT018159 suppresses ACTH synthesis and secretion in corticotroph tumor cells. CCT018159 also decreased cell proliferation and induced apoptosis. FACS analyses revealed that CCT018159 agents increased the percentage of AtT-20 cells in the G2/M phase. CCT018159 decreased cell proliferation, presumably due to the induction of cell death and arrest of the cell cycle in AtT-20 cells.[1] |
In vivo | CCT018159 (4 mg/mouse; s.c.; ones daily for 14 days; AtT-20-xenografted mice) reduced tumor weight compared to AtT-20-xenografted control mice. CCT018159 also decreased plasma ACTH levels, and POMC and PTTG1 mRNA levels in the tumor cells.[2] |
Molecular Weight | 352.38 |
Formula | C20H20N2O4 |
Cas No. | 171009-07-7 |
Smiles | CC1=C(C(=NN1)C2=CC(CC)=C(O)C=C2O)C=3C=C4C(=CC3)OCCO4 |
Relative Density. | 1.322 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 112.5 mg/mL (319.3 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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