KPT276, Inhibitor
KPT276
Purity
>98% (HPLC)
Synonyms
KPT276; KPT 276; KPT-276; inhibitor
Purity/Purification
>98% (HPLC)
Suitability
DMSO: 16mg/mL (37.5mM)
Ethanol: <1mg/mL
Water: <1mg/mL
Ethanol: <1mg/mL
Water: <1mg/mL
Target
CRM1
Receptor
CRM1
SMILES
C1C(CN1C(=O)/C=C1cnc(n1)c1cc(cc(c1)C(F)(F)F)C(F)(F)F)(F)F
Molecular Formula
C16H10F8N4O
CAS Number
1421919-75-6
Preparation and Storage
Store at -20 degree C
Stability: >=2 years
Shipping: Ice Pack
Stability: >=2 years
Shipping: Ice Pack
Related Product Information for KPT276, inhibitor
KPT-276 analog of KPT-185 is an orally bioavailable selective inhibitors of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of CRM1. IC50 value: Target: CRM1 in vitro: A selective inhibitor of nuclear export compound KPT-276 specifically and irreversibly inhibits the nuclear export function of XPO1. The viability of 12 HMCLs treated with KTP-276 was significantly reduced. KPT-276 also actively induced apoptosis in primary MM patient samples. In gene expression analyses two genes of probable relevance were dysregulated by KPT-276: cell division cycle 25 homolog A (CDC25A) and bromodomain-containing protein 4 (BRD4) both of which are associated with c-MYC pathway. Inhibition of CRM1 by two novel selective inhibitors of nuclear export (SINE) KPT-185 and KPT-276 in MCL cells resulted in significant growth inhibition and apoptosis induction. KPT-185 also induced CRM1 accumulation in the nucleus resulting in CRM1 degradation by the proteasome. in vivo: One week after leukemic cell inoculation the mice were given KPT-276 at 150mg/kg via oral gavage 3 times a week or vehicle control. KPT-276 has the identical CRM1 binding warhead and specificity as KPT-185 similar biologic activity in vitro but superior oral bioavailability and pharmacokinetics which allow it to be used in vivo. Mice were monitored for survival. Some mice were killed at day 21 to assess the effects of KPT-276 on leukemia burden by measuring spleen weight and white blood cell count. Oral administration of KPT-276 significantly suppressed tumor growth in an MCL-bearing severe combined immunodeficient mouse model without severe toxicity.
Product Categories/Family for KPT276, inhibitor
References
1.Ranganathan P et al. Blood. 2012 120 (9) 1765-1773.
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Product Notes
The KPT276 (Catalog #AAA3609402) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "KPT276, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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