5.31126
MPNST Inhibitor, Cpd21
Synonym(s):
MPNST Inhibitor, Cpd21, N-(Pyridin-3-yl)thiophene-2-carboxamide, Malignant Peripheral Nerve Sheath Tumors Inhibitor, Cpd 21
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About This Item
Empirical Formula (Hill Notation):
C10H8N2OS
CAS Number:
Molecular Weight:
204.25
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥97% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light beige
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
SMILES string
C1=CC(=CN=C1)NC(=O)C2=CC=CS2
InChI
1S/C10H8N2OS/c13-10(9-4-2-6-14-9)12-8-3-1-5-11-7-8/h1-7H,(H,12,13)
InChI key
UPLHUDRMLWWFRE-UHFFFAOYSA-N
General description
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.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Chau, V., et al. 2013. Cancer Res. 74, 586.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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