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1357470-29-1

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1357470-29-1 Usage

Uses

ON123300 is a potent multikinase inhibitor and may be potential useful for brain tumor chemotherapy. ON123300 strongly inhibits Ark5 and CDK4, as well as growth factor receptor tyrosine kinases.

Biological Activity

on123300 is a multi-targeted kinase inhibitor.the signaling hyperactivation of rtk is most commonly caused by egfr mutation/amplification or pdgfr amplification/overexpression. fgfr1signaling also occurs in gbm exhibiting fgfr1 kinase domain gain-of-function mutations.

in vitro

in previous study, when z138c and granta 519 cells were treated with on123300, it was found that on123300 was efficient to inhibit the phosphorylation of rb family proteins. moreover, on123300 was able to inhibit the phosphorylation of proteins that were involved in the pi3k/akt pathway. in addition, on123300-treated cells similarly arrested at lower concentrations, however, higher concentrations could lead to the apoptosis induction [1].

in vivo

previous animal in vivo study showed that mouse xenograft had a strong inhibition of mcl tumor growth in on123300-treated animals. moreover, the treatment with on123300 to ibrutinib-sensitive and -resistant patient-derived mcls was able to trigger apoptosis and inhibition of both rb and pi3k/akt pathways, indicating that on123300 could be an effective drug in the treatment of mcl, such as ibrutinib-resistant forms of the disease [1].

IC 50

3.9, 5, 26, 26, 9.2 and 11 nm for cdk4, ark5, pdgfrβ, fgfr1, ret, and fyn, respectively.

references

[1] divakar sk et al. dual inhibition of cdk4/rb and pi3k/akt/mtor pathways by on123300 induces synthetic lethality in mantle cell lymphomas. leukemia. 2016 jan;30(1):86-93.

Check Digit Verification of cas no

The CAS Registry Mumber 1357470-29-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,5,7,4,7 and 0 respectively; the second part has 2 digits, 2 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1357470-29:
(9*1)+(8*3)+(7*5)+(6*7)+(5*4)+(4*7)+(3*0)+(2*2)+(1*9)=171
171 % 10 = 1
So 1357470-29-1 is a valid CAS Registry Number.

1357470-29-1SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 17, 2017

Revision Date: Aug 17, 2017

1.Identification

1.1 GHS Product identifier

Product name ON123300

1.2 Other means of identification

Product number -
Other names 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1357470-29-1 SDS

1357470-29-1Downstream Products

1357470-29-1Relevant articles and documents

Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7- oxo-7,8-dihydro-pyrido[2,3- d ]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5)

Reddy, M. V. Ramana,Akula, Balireddy,Cosenza, Stephen C.,Athuluridivakar, Saikrishna,Mallireddigari, Muralidhar R.,Pallela, Venkat R.,Billa, Vinay K.,Subbaiah, D. R. C. Venkata,Bharathi, E. Vijaya,Vasquez-Del Carpio, Rodrigo,Padgaonkar, Amol,Baker, Stacey J.,Reddy, E. Premkumar

, p. 578 - 599 (2014/03/21)

The success of imatinib, a BCR-ABL inhibitor for the treatment of chronic myelogenous leukemia, has created a great impetus for the development of additional kinase inhibitors as therapeutic agents. However, the complexity of cancer has led to recent interest in polypharmacological approaches for developing multikinase inhibitors with low toxicity profiles. With this goal in mind, we analyzed more than 150 novel cyano pyridopyrimidine compounds and identified structure-activity relationship trends that can be exploited in the design of potent kinase inhibitors. One compound, 8-cyclopentyl-2-[4-(4-methyl- piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6- carbonitrile (7x), was found to be the most active, inducing apoptosis of tumor cells at a concentration of approximately 30-100 nM. In vitro kinase profiling revealed that 7x is a multikinase inhibitor with potent inhibitory activity against the CDK4/CYCLIN D1 and ARK5 kinases. Here, we report the synthesis, structure-activity relationship, kinase inhibitory profile, in vitro cytotoxicity, and in vivo tumor regression studies by this lead compound.

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