Name | 5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)-methyl]amino]-adenosine |
Synonyms | CS-1647 VER155008 VER 155008 VER-155008 VER 155088 8-(3,4-Dichlorobenzyl)aMino-5'-O-(4-cyanobenzyl)adenosine 5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine 5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)-methyl]amino]-adenosine 4-{(2R,3S,4R,5R)-5-[6-aMino-8-(3,4-dichlorobenzylaMino)purin-9-yl]-3,4-dihydroxytetrahydrofuran-2-ylMethoxyMethyl}benzonitrile 4-((((2R,3S,4R,5R)-5-(6-aMino-8-((3,4-dichlorobenzyl)aMino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)Methoxy)Methyl)benzonitrile |
CAS | 1134156-31-2 |
InChIKey | ZXGGCBQORXDVTE-UMCMBGNQSA-N |
Molecular Formula | C25H23Cl2N7O4 |
Molar Mass | 556.4 |
Density | 1.63±0.1 g/cm3(Predicted) |
Boling Point | 856.3±75.0 °C(Predicted) |
Solubility | DMSO: >10mg/mL |
Appearance | powder |
Color | white to light brown |
pKa | 13.04±0.70(Predicted) |
Storage Condition | 2-8°C |
MDL | MFCD18086892 |
In vitro study | VER-155008 inhibit the proliferation of human breast and colon cancer cell lines BT474,MB-468,HCT116, and HT29, GI50s ranges from 5.3-14.4 μm, and Hsp90 client protein degradation was induced in HCT116 and BT474 cells. In 8505C and FRO cells, VER-155008 time and dose dependently decreased cell viability and increased the percentage of dead cells. VER-155008 inhibited cytokine-dependent AML cell proliferation in a dose-dependent manner. VER-155008 showed potent inhibition of cell proliferation in A549 and H1975 cells. |
In vivo study | In HCT116 tumor-bearing mice, VER-155008 (25 or 40 mg/kg, I. v.) was rapidly metabolized and cleared with tumor levels below the predicted level of pharmacological activity. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.797 ml | 8.986 ml | 17.972 ml |
5 mM | 0.359 ml | 1.797 ml | 3.594 ml |
10 mM | 0.18 ml | 0.899 ml | 1.797 ml |
5 mM | 0.036 ml | 0.18 ml | 0.359 ml |
biological activity | VER155008 (C07) is a potent inhibitor of the Hsp70 family, and GRP78 (HSPA5, Bip) IC50 of 0.5 μm, 2.6 μm, and 2.6 μm, respectively, more than 100-fold higher than the HSP90 selectivity. VER155008 inhibits autophagy and results in reduced levels of HSP90 client proteins. |
Target | Value |
HSP70 (Cell-free assay) | 0.5 μM |
HSC70 (Cell-free assay) | 2.6 μM |
GRP78 (Cell-free assay) | 2.6 μM |
Use | an HSP70 inhibitor, IC50:500nM. |