KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity.
| Molecular Weight | 375.23 |
| Formula | C14H7F6N5O |
| CAS Number | 1388841-50-6 |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. |
| Felezonexor (CBS9106)
Felezonexor (CBS9106; SL-801) is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity without affecting CRM1 mRNA levels. 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. |
| 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. |
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