1542705-92-9
1542705-92-9 structure
- Name: CB-5083
- Chemical Name: CB-5083
- CAS Number: 1542705-92-9
- Molecular Formula: C24H23N5O2
- Molecular Weight: 413.472
- Catalog: Signaling Pathways Cell Cycle/DNA Damage p97
- Create Date: 2018-03-22 14:30:50
- Modify Date: 2024-01-06 18:25:08
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CB-5083 is a potent, selective and orally bioavailable p97 inhibitor with an IC50 value of 11 nM.
| Name | CB-5083 |
|---|---|
| Synonyms |
1H-Indole-4-carboxamide, 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-
1-[4-(Benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-1H-indole-4-carboxamide |
| Description | CB-5083 is a potent, selective and orally bioavailable p97 inhibitor with an IC50 value of 11 nM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 11 nM (p97)[1] |
| In Vitro | Treatment of tumor cells with CB-5083 leads to significant accumulation of markers associated with inhibition of ubiquitin−proteasome system and endoplasmic reticulum-associated degradation functions, which induces irresolvable proteotoxic stress and cell death[1] |
| In Vivo | In tumor bearing mice, oral administration of CB-5083 causes rapid accumulation of markers of the unfolded protein response and subsequently induces apoptosis leading to sustained antitumor activity in in vivo xenograft models of both solid and hematological tumors. CB-5083 has been taken into phase 1 clinical trials in patients with multiple myeloma and solid tumors[1]. |
| Kinase Assay | The ATPase assay is performed to determine the IC50 value. compounds (CB-5083) are diluted in DMSO with a 3-fold 10-point serial dilution starting at 10 μM. The assay is done in a 384-well plate with each row as a single dilution |
| Cell Assay | A549 and other tumor cell lines are cultured according to ATCC guidelines. Cells are cultured in black or white, clear-bottomed, tissue culture-treated 384-well plates. Cells are treated with 10-point dose titration of the compound (CB-5083) in well duplicates. After a 72 h treatment, CellTiter-Glo is added to the white plates to measure cell viability[1]. |
| Animal Admin | Mice: Tumor-bearing mice are used to evaluate pharmacokinetics and pharmacodynamics effect and antitumor activity. Both molecules (CB-5083 and compoud 69) are administered orally as a suspension in 0.5% methylcellulose aqueous suspensions at the fixed dose strength of 150 mg/kg; plasma and tumor samples at multiple time points (2, 6, 16, and 24 h) are harvested for pharmacokinetics and pharmacodynamics analysis[1]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 760.5±70.0 °C at 760 mmHg |
| Molecular Formula | C24H23N5O2 |
| Molecular Weight | 413.472 |
| Flash Point | 413.8±35.7 °C |
| Exact Mass | 413.185181 |
| LogP | 2.61 |
| Vapour Pressure | 0.0±2.6 mmHg at 25°C |
| Index of Refraction | 1.710 |
| Storage condition | -20℃ |