Felezonexor (CBS9106; SL-801) is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity without affecting CRM1 mRNA levels. This effect could be reversed by adding bortezomib or LMB. Felezonexor (CBS9106) inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells, including multiple myeloma cells.
Felezonexor is also a reversible inhibitor of XPO1, inhibits nuclear export by covalently binding to Cys528 as well as by inducing the degradation of XPO1.
Oral administration of Felezonexor (CBS9106) significantly suppresses tumor growth and prolongs survival in mice bearing tumor xenograft without a significant loss in body weight. A reduced level of CRM1 protein is also observed in tumor xenografts isolated from mice treated with Felezonexor (CBS9106).
| Molecular Weight | 419.83 |
| Formula | C18H21ClF3N3O3 |
| CAS Number | 1076235-04-5 |
| 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.
| Related CRM1 Products |
|---|
| CRM1-IN-2
CRM1-IN-2 is a noncovalent CRM1 inhibitor. |
| CRM1-IN-1
CRM1-IN-1 is a noncovalent CRM1 inhibitor. |
| KPT-251
KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity. |
| Eltanexor
Eltanexor, also known as KPT-8602, is a second-generation exportin-1 (CRM1) inhibitor with IC50 values of 20−211 nM in 10 AML lines. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
