Key Specifications Table
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|5.31126.0001||Glass bottle||25 mg|
|Overview||A cell-permeable, bioavailable, non-toxic pyridinylthiophene-carboxamide compound that preferentially and reversibly inhibits the growth of malignant peripheral nerve sheath tumors (MPNSTs) in both human and murine models in a dose-dependent manner (EC50 = 439 nM, 754 nM, and 1.0 µM in S462, SNF96.2, and sMPNST cells). Exhibits toxicity towards neurofibromatosis type 1 (Nf1) and p53 deficient MPNST cells, but does not affect normally dividing Schwann cells and mouse embryonic fibroblasts. Shown to reduce ATP consumption by all MPNST cells studied (EC50 = 1.0 µM). Synergizes with PI-3 Kinase inhibitor, LY-294002 (Cat. Nos. 440202 & 440204) to block the growth of MPNST cells. Reduces the expression of cyclin A2, B1, D1, E, cdk4, and cdk6 and increases the expression of cdkn1a and cdkn2a in a dose dependent manner. Blocks cell cycle at G1/S phase leading to apoptosis in cancer cells. Displays favorable pharmacokinetic profile and is rapidly distributed from the plasma into sMPNST tissues and has a half-life of 6-8 hours in sMPNST tissue following its complete distribution. Reduces MPNST burden in a mouse allograft model and enhances survival (~40 mg/kg, i.p. in mice for 4 weeks).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
|Synonyms||N-(Pyridin-3-yl)thiophene-2-carboxamide, Malignant Peripheral Nerve Sheath Tumors Inhibitor, Cpd 21|
|References||Chau, V., et al. 2013. Cancer Res. 74, 586.|
|Form||Light beige solid|
|Purity||≥97% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
MPNST Inhibitor, Cpd21 - Calbiochem SDS
|Chau, V., et al. 2013. Cancer Res. 74, 586.|
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.