Home Transmembrane Transporters CRM1 inhibitor KPT-276 For research use only.

KPT-276

KPT-276 is an orally bioavailable selective CRM1 inhibitor.

KPT-276 Chemical Structure

KPT-276 Chemical Structure

CAS No. 1421919-75-6

Purity & Quality Control

Batch: S725101 DMSO]20 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.45%
99.45

KPT-276 Related Products

Biological Activity

Description KPT-276 is an orally bioavailable selective CRM1 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
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
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]
Animal Research Animal Models Human leukemia (MV4-11) xenografts are established in mice.
Dosages ~150 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 426.26 Formula

C16H10F8N4O
CAS No. 1421919-75-6 SDF Download KPT-276 SDF
Smiles C1C(CN1C(=O)C=CN2C=NC(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 20 mg/mL ( (46.91 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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