CCT 018159
Synonym(s):4-(4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-methyl-1H-pyrazol-3-yl)-6-ethylresorcinol;HSP90 Inhibitor, CCT018159 - CAS 171009-07-7 - Calbiochem
- CAS NO.:171009-07-7
- Empirical Formula: C20H20N2O4
- Molecular Weight: 352.38
- MDL number: MFCD00710300
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:12
What is CCT 018159?
The Uses of CCT 018159
CCT 018159 is a cell-permeable compound that inhibits Hsp90 ATPase.
What are the applications of Application
CCT 018159 is a cell-permeable compound that inhibits Hsp90 ATPase
Definition
ChEBI: A member of the class of pyrazoles that is 1H-pyrazole carrying 1,4-benzodioxane-6-yl and 5-ethyl-2,4-dihydroxyphenyl substituents at positions 4 and 5 respectively.
Biological Activity
Novel inhibitor of heat shock protein 90 (Hsp90) ATPase activity (IC 50 = 5.7 μ M) that displays selectivity over human Hsp72 and topoisomerase II. Inhibits proliferation of HCT116 human colon tumor cells and produces upregulation of Hsp70 and downregulation of c-Raf and cdk4. More soluble than 17-AAG (17-Demethoxy-17-(2-propenylamino)geldanamycin ) and is independent of NQO1/DT-diaphorase and P-glycoprotein expression.
in vitro
cct018159 was identified by high-throughput screening inhibiting human hsp90beta with comparable potency to 17-aag and with similar atp-competitive kinetics. x-ray crystallographic structures of the yeast hsp90 complexed with cct018159 showed binding properties similar to radicicol. the mean cellular gi50 of cct018159 across a panel of human cancer cell lines, including melanoma, was 5.3 μm. unlike 17-aag, the in-vitro antitumor activity of cct018159 was independent of nqo1/dt-diaphorase and p-glycoprotein expression. the signature of hsp90 inhibition, comprising increased expression of hsp72 protein and depletion of erbb2, cdk4, c-raf, and mutant b-raf, was indicated in human cancer cell lines treated with cct018159 [1].
in vivo
in human tumor xenografts including skmel 28 melanoma cells, cct018159 was found to induce the expression of hsp72 as well as erbb2, cdk4 and dc-raf [1].
storage
Store at +4°C
References
[1] s. y. sharp, k. boxall, m. rowlands, et al. in vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors. cancer research 67(5), 2206-2216 (2007).
Properties of CCT 018159
Boiling point: | 547.3±50.0 °C(Predicted) |
Density | 1.322±0.06 g/cm3(Predicted) |
storage temp. | Store at +4°C |
solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
pka | 8.84±0.48(Predicted) |
form | White solid |
color | White to off-white |
Safety information for CCT 018159
Computed Descriptors for CCT 018159
New Products
6-Bromo 2-Iodo Indole Pyridine 2,4,6-Tricarboxaldehyde Fosfomycin EP impurity D Rimegepant Impurity 3 Ivermectin EP Impurity B 2,2-diethoxyethanethioamide Tubulysin C Tubulysin E 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile Imeglimin Hydrochloride IH (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Calcium Sodium Phosphosilicate IH 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate Methyl 4-amino-3-(4-phenylpiperazin-1-yl)benzoate Diethyl 2,5-di(furan-2-yl)terephthalate (1-Isopropyl-1H-pyrazol-5-yl)boronic acid Methyl 4-amino-3-(piperidin-1-yl)benzoate 2-(4-Bromopyridin-2-yl)acetonitrile 3,6-Bis(4-iodophenyl)-2,5-dihydropyrrolo[3,4-c]pyrrole-1,4-dione 4,6-difluoro-1H-indole 6-bromopyridazin-3-amine Boronic acid, [4-(2-aminoethyl)phenyl] 2-(2,5-Dihydrofuran-3-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolaneRelated products of tetrahydrofuran
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