Hantzsch ester – PT1 small molecule (tool compound)

Contributors

Inventor	Institute
Chris Jones	Queen Mary University of London

Additional notes:	>95 % purity
Molecular weight:	359.42

Storage conditions:	4° C
Solubility:	DMSO, CH2Cl2, EtOAc

References:	DOI: 10.1055/s-0037-1611065 Trinchera et al. 2017. Org Lett. 19(17):4644-4647. PMID: 28817286. Intermolecular Aryne Ene Reaction of Hantzsch Esters: Stable Covalent Ene Adducts from a 1,4-Dihydropyridine Reaction.

Unfortunately this tool is not available through our online checkout process. Please contact our team directly to obtain further information on accessing this tool.

Enquire about this Tool

If you are a for-profit organisation or a researcher working on commercially-sponsored academic research, you will need to contact our licensing team for a commercial use license.

Request a license

Get technical support

New to CancerTools?

We are a trusted, non-profit platform for cancer research products, part of Cancer Research UK – by sourcing your cancer research tools from us you help fund future cancer research.

Find out more

Related Tools for Small molecules

Cat. #

Tool Name

151712

CDK7 inhibitor BS-181 Small Molecule (Tool Compound)

Key Info

Cat. #:	151712
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	BS-181 is stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. BS-181 inhibits the growth of MCF-7 xenografts in the nude mice model in a dose-dependent manner, with 25% and 50% reduction in tumor growth after 2 weeks of treatment at 10 mg/kg/day and 20 mg/kg/day, respectively without apparent toxicity. BS-181 is a small molecule inhibitor of CDK7 in a cell-free environment, which displays more potential activity than roscovitine with IC 50 of 510 nM. Among the CDKs and other 69 kinases from many different classes, BS-181 shows high inhibitory selectivity for CDK7, inhibits CDK2 at concentrations lower than 1 ÎźM which being inhibited 35-fold less potently (IC50 with 880 nM) than CDK7, shows slight inhibition for CDK1, CDK4, CDK5, CDK6 and CDK9 with IC50 values higher than 3.0 ÎźM, and only shows inhibition for several kinases from other classes at high concentrations (>10 ÎźM). BS-181 promotes cell cycle arrest and inhibits the cancer cell growth of a range of tumor types, including breast, lung, prostate and colorectal cancer with IC50 in the range of 11.5-37 ÎźM. In MCF-7 cells, BS-181 inhibits the phosphorylation of the CDK7 substrate RNA polymerase II COOH-terminal domain (CTD), and promotes cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines.

View Tool

151831

Protein Kinase D inhibitor CRT0066101 Small Molecule (Tool Compound)

Key Info

Cat. #:	151831
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	In Panc-1 subcutaneous xenograft model, orally administration of CRT0066101 at the dosage of 80 mg/kg/d for 24 days significantly suppressed pancreatic cancer growth. Moreover, when CRT0066101 reached its peak concentration (12 Îźmol/L) in tumor model, the expression of activated PKD1/2 in the treated tumor explants was substantially decreased. It was concluded that CRT0066101 given orally at 80 mg/kg/d for 21 days in Panc-1 orthotropic model suppressed tumor growth potently in vivo. Clinical…

View Tool

152709

Dual DNA-PK/PI3K inhibitor KU-0060648 Small Molecule (Tool Compound)

Key Info

Cat. #:	152709
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model. KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only b…

View Tool

152786

Nucleolar Luminophore Ag-1 Small Molecule (Tool Compound)

Key Info

Cat. #:	152786
Sub-type:	Luminophore
Availability:	Please enquire for quantities and pricing

View Tool

152788

Phosphatidylinositol-4-phosphate 5-kinase inhibitor PIP5K Small Molecule (Collaborative Toolkit)

Key Info

Cat. #:	152788
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing

View Tool

By Category

By Cancer Type

More

Hantzsch ester – PT1 small molecule (tool compound)

Contributors

Related Tools for Small molecules

Tool enquiry