VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
| Cell Experiment | |
|---|---|
| Cell lines | Melanoma cells (SKMEL 2, SKMEL 5, SKMEL 28, WM266.4); Colon cancer cells (HCT116, BEneg, BE2, HT29, HT29oxaliR); Ovarian cancer cells (CH1, CH1doxR); Breast cancer cells (MB-231, MB-468, BT20, ZR751, MCF7, BT-474); nontumorigenic cells (HUVEC, MCF10a, PNT |
| Preparation method | Using the sulforhodamine B assay to mearsure antiproliferative effects . Determining HUVEC sensitivity by an alkaline phosphatase method. |
| Concentrations | ~10 μM |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | Mice bearing established OVCAR3 human ovarian xenografts |
| Formulation | 10% DMSO, 5% Tween 20, 85% saline |
| Dosages | ~4 mg/kg |
| Administration | i.p. |
| Molecular Weight | 387.82 |
| Formula | C19H18ClN3O4 |
| CAS Number | 940289-57-6 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[5] Xavier Barril, et al. 4-Amino derivatives of the Hsp90 inhibitor CCT018159
| Related HSP Products |
|---|
| Hsp70-derived octapeptide
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs. |
| p5 Ligand for Dnak and DnaJ
p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. |
| Tertomotide hydrochloride
Tertomotide hydrochloride is a peptide consisting of 16 amino acids containing sequences derived from human telomerase reverse transcriptase (TERT).Tertomotide penetrates cells and interacts with HSP70 and HSP90, as well as inhibiting amyloid beta and tau, and inhibiting aging-related signaling in the brain. pathways, which could be used in aging and Alzheimer's disease related studies. |
| BMS-986263
BMS-986263 is a small interfering RNA (siRNA) that targets Hsp47 and can be used in studies related to idiopathic pulmonary fibrosis (IPF). |
| AT-533
AT-533 is a potent Hsp90 and HSV inhibitor. |
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