SW106065

Modify Date: 2024-01-12 12:21:28

SW106065 Structure
SW106065 structure
Common Name SW106065
CAS Number 62289-81-0 Molecular Weight 204.24800
Density N/A Boiling Point N/A
Molecular Formula C10H8N2OS Melting Point N/A
MSDS N/A Flash Point N/A

 Use of SW106065


SW106065 is an apoptosis inducer in malignant peripheral nerve sheath tumors (MPNST). SW106065 inhibits ATP consumption of sMPNST and other models of MPNST with an EC50 of 1 µM. SW106065 can be used for MPNST research[1].

 Names

Name N-pyridin-3-ylthiophene-2-carboxamide
Synonym More Synonyms

 SW106065 Biological Activity

Description SW106065 is an apoptosis inducer in malignant peripheral nerve sheath tumors (MPNST). SW106065 inhibits ATP consumption of sMPNST and other models of MPNST with an EC50 of 1 µM. SW106065 can be used for MPNST research[1].
Related Catalog
In Vitro SW106065 (Compound 21, Cpd21) inhibits the human MPNST cell lines growth in a dose-dependent manner, and EC50 concentrations of 439 nM and 753.6 nM for S462 and SNF96.2 cells, respectively. SW106065 remains nontoxic to normally dividing Schwann cells or mouse embryonic fibroblasts[1]. SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment shows a decreased percentage of cells in S phase, and a corresponding increased percentage in G1/G0 and G2/M[1]. SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment decreases the levels of cyclin A2, cyclin B1, cyclin D1, cyclin E, cdk4, and cdk6. And increases levels of cdkn1a and cdkn2a mRNA were observed in a dose-dependent manner.SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment decreases the levels of Cyclin D1 protein[1]. SW106065 (Cpd21) treatment significant increase in the percentage of apoptotic cells[1]. Cell Cycle Analysis[1] Cell Line: sMPNST cells Concentration: 0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM Incubation Time: 24 hours Result: Showed a decreased percentage of cells in S phase, and a corresponding increased percentage in G1/G0 and G2/M. RT-PCR[1] Cell Line: sMPNST cells Concentration: 0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM Incubation Time: 24 hours Result: Decreased levels of cyclin A2, cyclin B1, cyclin D1, cyclin E, cdk4, and cdk6. Increased levels of cdkn1a and cdkn2a mRNA were observed in a dose-dependent manner. Western Blot Analysis[1] Cell Line: sMPNST cells Concentration: 0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM Incubation Time: 24 hours Result: Decreased levels of Cyclin D1 protein.
In Vivo SW106065 (Cpd21; 40 mg/kg; intraperitoneal injection; twice per day for 4 weeks) treatment can be delivered to mice in concentrations to sufficiently penetrate sMPNST tissue, and inhibit tumor development[1]. Animal Model: NCR-nu/nu female mice (6-7 week old) injected with MPNST cells[1] Dosage: 40 mg/kg Administration: Intraperitoneal injection; twice per day for 4 weeks Result: Reduced MPNST burden in a mouse allograft model.
References

[1]. Vincent Chau, et al. Preclinical therapeutic efficacy of a novel pharmacologic inducer of apoptosis in malignant peripheral nerve sheath tumors. Cancer Res. 2014 Jan 15;74(2):586-97.

 Chemical & Physical Properties

Molecular Formula C10H8N2OS
Molecular Weight 204.24800
Exact Mass 204.03600
PSA 70.23000
LogP 2.46840

 Synonyms

N-(3-pyridinyl)-2-thiophenecarboxamide
thiophene-2-carboxylic acid pyridin-3-ylamide
SW-106065