[CAS NO. 1421919-75-6] KPT-276
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PRODUCTS SPECIFICATIONS [1421919-75-6]
Store
Catalog
SLK-S7251
Brand
Selleck
CAS
1421919-75-6
DESCRIPTION [1421919-75-6]
Overview
| MDL | MFCD27937049 |
|---|---|
| Molecular Weight | 426.26 |
| Molecular Formula | C16H10F8N4O |
| SMILES | O=C(N1CC(F)(F)C1)/C=C\N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3460 mL | 11.7299 mL | 23.4599 mL |
| 5 mM | 0.4692 mL | 2.3460 mL | 4.6920 mL |
| 10 mM | 0.2346 mL | 1.1730 mL | 2.3460 mL |
| 50 mM | - | - | - |
Description
KPT-276 is an orally bioavailable selective inhibitor.
Features
Superior oral bioavailability and PK profile relative to KPT-185 in vivo. Potential for use in hematological malignancies such as AML and multiple myeloma.
Targets
| CRM1 [1] |
In vitro
KPT-276 results in significant growth inhibition and apoptosis induction in MCL cells. KPT-276 specifically and irreversibly inhibits the nuclear export function of XPO1, and reduces the viability of 12 HMCLs. KPT-276 also actively induces apoptosis in primary MM patient samples.
In vivo
KPT-276 significantly prolongs survival of leukemic mice and reduces leukemic burden in a xenograft AML mouse model. KPT-276 significantly suppresses tumor growth in an MCL-bearing severe combined immunodeficient mouse model without severe toxicity. KPT-276 reduces monoclonal spikes in the Vk*MYC transgenic MM mouse model, and inhibits tumor growth in a xenograft MM mouse model.
References
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