Poly(ethylene glycol)poly(lysine) block copolymerubenimex conjugate small molecule (tool compound)

The molecule exerts stronger inhibitory effect at lower concentrations that Ube alone,suggesting that PLys conjugation effectively increases the antitumor effect in HCC cells, presumably by targeting APN/CD13+cells, and enhances the strength of molecule-to-cell interactions.

Contributors

Inventor	Institute
Masaki Mori ; Hideshi Ishii ; Masamitsu Konno ; Hidetoshi Eguchi ; Naotsgu Haraguchi ; Reishi Toshiyama ; Nobuhiro Nishiyama ; Hiroyasu Takemoto – Osaka University ; Tokyo Institute of Technology ; Tokyo Institute of Technology	Osaka University ; Tokyo Institute of Technology

Cat. #:	156495
Tool sub type:	Inhibitor
Research Fields:	Drug development

Product description:	The molecule exerts stronger inhibitory effect at lower concentrations that Ube alone,suggesting that PLys conjugation effectively increases the antitumor effect in HCC cells, presumably by targeting APN/CD13+cells, and enhances the strength of molecule-to-cell interactions.

Primary target:	This conjugate targets aminopeptidase N and exerts an antitumor effect in hepatocellular carcinoma stem cells

Shipping conditions:	Dry Ice

References:	Toshiyama et al. 2019. Oncogene. 38(2):244-260. PMID: 30089817.

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

151834

Antitumoral Quinol1h Small Molecule (Tool Compound)

Key Info

Cat. #:	151834
Sub-type:	Antitumoral
Availability:	Please enquire for quantities and pricing
Application:	Antitumor activity observed in HCT 116 (GI50 = 40 nM) and HT 29 (GI50 = 380 nM), and in breast cancer cell lines. Potent inhibitory effect in NCI 60 cells (GI50 =16 nM and LC50 = 2.24 ÂľM).

View Tool

151889

DNA-PK inhibitor NU7441 Small Molecule (Tool Compound)

Key Info

Cat. #:	151889
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases etoposide-induced tumor growth delay 2-fold in mice bearing SW620 xenografts. NU7441 increases the persistence of ÎłH2AX foci after ionizing radiationâinduced or etoposide-induced DNA damage. NU7441 (0.5 ÎźM or 1 ÎźM) appreciably increases G2-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. NU7441 causes persistence of d…

View Tool

152625

Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)

Key Info

Cat. #:	152625
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	CCT251455 displays a favorable oral pharmacokinetic profile, shows dose-dependent inhibition of MPS1 in an HCT116 human tumor xenograft model, and is an attractive tool compound to elucidate further the therapeutic potential of MPS1 inhibition. In Female Balb/C mice it had an oral bioavailabilty of 83%.

View Tool

152754

CDK2 inhibitor NU6301 Small Molecule (Tool Compound)

Key Info

Cat. #:	152754
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	The prodrug NU6301 rapidly generated NU6102 in vitro in mouse plasma, and tumour NU6102 levels in vivo consistent with activity in vitro. Eight or 12 hourly dosing of 120 mg/kg NU6301 for 10 days was well tolerated in SKUT-1B tumour-bearing mice and inhibited Rb phosphorylation in tumour tissue. Two (8 hourly dosing) and 3 (12 hourly dosing) day tumour growth delay was observed (p=0.04 and p=0.007, respectively) following NU6301 administration. NU6102 selectively inhibited the growth of CDK2 WT (wild type) versus KO MEFs (knockout mouse embryo fibroblasts) (GIââ (concentration required to inhibit cell growth by 50%) 14 ÎźM versus >30 ÎźM), and was more growth-inhibitory in p53 mutant or null versus p53 WT cells (p=0.02), and in Rb (retinoblastoma protein) WT SKUT-1B versus SKUT 1 Rb deficient cells (p=0.01). In SKUT-1B cells NU6102 induced a G2 arrest, inhibition of Rb phosphorylation and cytotoxicity (LCââ 2.6 ÎźM for a 24h exposure).

View Tool

By Category

By Cancer Type

More

Poly(ethylene glycol)poly(lysine) block copolymerubenimex conjugate small molecule (tool compound)

Contributors

Related Tools for Small molecules

Tool enquiry