KPT-276

Catalog No.S7251 Batch:S725101

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Technical Data

Formula

C16H10F8N4O
Molecular Weight 426.26 CAS No. 1421919-75-6
Solubility (25°C)* In vitro DMSO 20 mg/mL (46.91 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
30%PEG400 0.5%Tween80 5%propylene glycol
5.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 16.67 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O Dilute to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description KPT-276 is an orally bioavailable selective CRM1 inhibitor.
Targets
CRM1 [1]
In vitro KPT-276 results in significant growth inhibition and apoptosis induction in MCL cells. [2] 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. [3]
In vivo KPT-276 significantly prolongs survival of leukemic mice and reduces leukemic burden in a xenograft AML mouse model. [1] KPT-276 significantly suppresses tumor growth in an MCL-bearing severe combined immunodeficient mouse model without severe toxicity. [2] KPT-276 reduces monoclonal spikes in the Vk*MYC transgenic MM mouse model, and inhibits tumor growth in a xenograft MM mouse model. [3]
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.

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Human leukemia (MV4-11) xenografts are established in mice.

  • Dosages

    ~150 mg/kg

  • Administration

    Oral gavage

Selleck's KPT-276 has been cited by 4 publications

Traumatic injury compromises nucleocytoplasmic transport and leads to TDP-43 pathology [ Elife, 2021, 10e67587] PubMed: 34060470
Transcriptome Profiling of Acquired Gefitinib Resistant Lung Cancer Cells Reveals Dramatically Changed Transcription Programs and New Treatment Targets [ Front Oncol, 2020, 10:1424] PubMed: 32923394
Modulation of actin polymerization affects nucleocytoplasmic transport in multiple forms of amyotrophic lateral sclerosis. [ Nat Commun, 2019, 10(1):3827] PubMed: 31444357
The C9orf72 repeat expansion disrupts nucleocytoplasmic transport [Zhang K Nature, 2015, 525(7567):56-61] PubMed: 26308891

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.