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1357470-29-1 (ON123300)

1

Identification

ON123300 ON123300
Name ON123300
Formula C24H27N7O
MW 429.52
CAS No. 1357470-29-1
EINECS
Smiles N#CC1=CC2=CN=C(NC3=CC=C(N4CCN(C)CC4)C=C3)N=C2N(C5CCCC5)C1=O
Synonyms ON 123300;ON-123300; 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile
InChI InChI=1S/C24H27N7O/c1-29-10-12-30(13-11-29)20-8-6-19(7-9-20)27-24-26-16-18-14-17(15-25)23(32)31(22(18)28-24)21-4-2-3-5-21/h6-9,14,16,21H,2-5,10-13H2,1H3,(H,26,27,28)
2

Introduction

Leukemia. 2016 Jan;30(1):86-93. Cancer Res. 2016 Mar 1;76(5):1225-36. Mol Cancer Ther. 2014 May;13(5):1105-16.

Background Information

In vitro: ON123300 is a novel kinase inhibitor, inhibits CDK4/6 and PI3K-δ and exhibits potent activity against mantle cell lymphomas (MCLs). ON123300 is a low molecular weight multi-kinase inhibitor identified through a series of screens that supported further analyses for brain tumor chemotherapy. Biochemical assays indicated ON123300 was a strong inhibitor of Ark5 and CDK4 as well as growth factor receptor tyrosine kinases such as Beta-type platelet-derived growth factor receptor [PDGFRβ]. ON123300 inhibited U87 glioma cell proliferation with an IC50 = 3.4 ± 0.1 μM and reduced phosphorylation of Akt, yet it also unexpectedly induced Erk activation; both in a dose- and time-dependent manner that subsequently was attributed to relieving Akt-mediated C-Raf S259 inactivation and activating a p70S6K initiated PI3K negative feedback loop. ......by AbMole BioScience
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 such as ??-type platelet-derived growth factor receptor (PDGFR??). ......by AdooQ BioScience, LLC
ON123300, a dihydropyrido[2,3-d]pyrimidine derivative, has been found to be an effective multikinase inhibitor that could be probably used against brain tumor and mantle cell lymphomas. It is still under preclinical trials in Colorectal cancer. IC50: 3.8 ......by BOC Sciences
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 such as β-type platelet-derived growth factor receptor (PDGFRβ). ON123300 inhibits U87 glioma cell proliferation with an IC(50) 3.4 ± 0.1 μmol/L. ON123300 exhibits potent activity against mantle cell lymphomas (MCLs) both in vitro and in vivo. ON123300 might be an effective agent in MCL, including ibrutinib-resistant forms of the disease. ......by MedKoo Biosciences, Inc.
ON123300 is a potent, multi-targeted kinase inhibitor with IC50 of 5, 3.9, 26, 26, 9.2 and 11 nM for ARK5, CDK4, PDGFRβ, FGFR1, RET and FYN, respectively; inhibits U87 glioma cell proliferation with IC50 3.4 uM, and reduces phosphorylation of Akt, yet it also unexpectedly induces Erk activation and prevents phosphorylation of C-Raf S259; suppresses phosphorylation of Akt as well as activation of Erk in brain tumors in vivo; also exhibits potent activity against mantle cell lymphomas both in vitro and in vivo, triggers apoptosis and inhibition of the Rb and PI3K/AKT pathways. ......by ProbeChem
ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5, PDGFRβ, FGFR1, RET, and Fyn, respectively. ......by Selleck Chemicals LLC
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:Off-white to orange Solid EBNumber:EB000071871

Storage condition

Solubility

10 mM in DMSO by CHEMSCENE, LLC
10 mM in DMSO by MedChemexpress Co., Ltd.
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Mechanism and Indication

Signaling Pathways Cell Cycle/DNA Damage
Target CDK
Research Area Cancer
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
ON123300 - No Development Reported
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Safety Data of ON123300

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD144();10mg/USD216() USA
Cayman Chemical Company USA
MedChemexpress Co., Ltd. 5mg/USD144();10mg/USD216() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD144();10mg/USD216() China
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Related Products

Other Forms of 1357470-29-1

Name CAS No Formula MW

Recommended Compounds in CDK

Name CAS No Formula MW
LY2857785 1619903-54-6 C26H36N6O 448.6
THZ2 1604810-84-5 C31H28ClN7O2 566.0527
Palbociclib (isethionate) 827022-33-3 C26H35N7O6S 573.66
CDK9-IN-6 1391855-95-0 C27H37ClN6O2 513.07468
ML167 1285702-20-6 C19H17N3O3 335.36
AMG 925 1401033-86-0 C26H29N7O2 471.55
LDC000067 1073485-20-7 C18H18N4O3S 370.43
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 570.64
LEE011 (succinate) 1374639-75-4 C27H36N8O5 552.63
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 471.0
LEE011 1211441-98-3 C23H30N8O 434.54
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
Wogonin 632-85-9 C16H12O5 284.26
1-NM-PP1 221244-14-0 C20H21N5 331.41
WHI-P180 211555-08-7 C16H15N3O3 297.31
THZ1 1604810-83-4 C31H28ClN7O2 566.05
Senexin A 1366002-50-7 C17H14N4 274.32
CDK4-IN-1 1256963-02-6 C22H29ClN8 440.97
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99
Purvalanol B 212844-54-7 C20H25ClN6O3 432.9

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

13

More Information

ON123300

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