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784210-88-4 (RGB-286638 (free base))

1

Identification

RGB-286638 (free base) RGB-286638 (free base)
Name RGB-286638 (free base)
Formula C29H35N7O4
MW 545.63
CAS No. 784210-88-4
EINECS
Smiles O=C(NN1CCOCC1)NC2=CC=CC(C3=C4C(C5=CC=C(CN6CCN(CCOC)CC6)C=C5)=NN3)=C2C4=O
Synonyms 1-(3-(4-((4-(2-methoxyethyl)piperazin-1-yl)methyl)phenyl)-4-oxo-1,4-dihydroindeno[1,2-c]pyrazol-5-yl)-3-morpholinourea
InChI InChI=1S/C29H35N7O4/c1-39-16-13-34-9-11-35(12-10-34)19-20-5-7-21(8-6-20)26-25-27(32-31-26)22-3-2-4-23(24(22)28(25)37)30-29(38)33-36-14-17-40-18-15-36/h2-8H,9-19H2,1H3,(H,31,32)(H2,30,33,38)
2

Introduction

Cyclin-dependent kinase

Background Information

Novel multitargeted cyclin-dependent kinase inhibitor, triggering P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs ......by AOBIOUS INC
RGB-286638 free base is a novel CDK inhibitor. It inhibited several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. It demonstrated equimolar (50nM) activity in freshly isolated tumor cells from MM patients, while manif ......by BOC Sciences
RGB-286638 is a potent and selective cyclin-dependent kinase (CDK) inhibitor with IC₅₀ values of 1, 2, 3 and 44 nM for CDK9, CDK1, CDK2, and CDK4, respectively. Less potent against cyclin H-CDK7 and cyclin D3-CDK6. It inhibits cell cycle progression in cancer cells by targeting CDKs, and is also found to induce apoptosis. In a range of pre-clinical models of solid and hematological tumors, RGB-286638 treatment results in tumor regression and increased survival. ......by BioVision, Inc.,
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM. ......by MedChemexpress Co., Ltd.
RGB-286638 is a multitargeted cyclin-dependent kinase inhibitor. RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. GB-286638 treatment resulted in MM cytotoxicity in vitro associated with inhibition of MM tumor growth and prolonged survival in vivo. RGB-286638 displayed caspase-dependent apoptosis in both wt-p53 and mutant-p53 cells that was closely associated with the downregulation of RNA polymerase II phosphorylation and inhibition of transcription. RGB-286638 triggered p53 accumulation via nucleolar stress and loss of Mdm2, accompanied by induction of p53 DNA-binding activity. ......by MedKoo Biosciences, Inc.
RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6. ......by Target Molecule Corp.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000017669

Storage condition

4°C by MedChemexpress Co., Ltd.

Solubility

DMSO:35mg/mL by CHEMSCENE, LLC
DMSO:35mg/mL by MedChemexpress Co., Ltd.
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Mechanism and Indication

Signaling Pathways Cell Cycle/DNA Damage
Target CDK
Research Area Cancer
Indications Hematological Malignancies
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
RGB-286638 (free base) Agennix Hematological Malignancies 2010/7/20 Phase 1 Clinical
RGB-286638 (free base) - Withdrawn
RGB-286638 (free base) - No Development Reported
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Safety Data of RGB-286638 (free base)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC USA
Apexbio Technology LLC 5mg/USD333() USA
Ark Pharm, Inc. USA
Arking Pharma 1g/USD3500() Canada
BOC Sciences
BioVision, Inc., 5mg/USD165() USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD180();10mg/USD300() USA
MedChemexpress Co., Ltd. 5mg/USD180();10mg/USD300() USA
MedKoo Biosciences, Inc. USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD180();10mg/USD300() China
Target Molecule Corp. 2mg/USD116();5mg/USD145();10mg/USD242();50mg/USD1078() USA
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Related Products

Other Forms of 784210-88-4

Name CAS No Formula MW
RGB-286638 784210-87-3 C29H37Cl2N7O4 618.55

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
RGB-286638 784210-87-3 C29H37Cl2N7O4 618.55
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Route of Synthesis

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References

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More Information

RGB-286638 (free base)

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