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RGB-286638 (free base)

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.

Product Specifications

CAS Number

[784210-88-4]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

CDK; GSK-3; JAK; MEK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/RGB-286638-free-base.html

Purity

98.87

Solubility

DMSO : 2.6 mg/mL (ultrasonic) |Ethanol : < 1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NN1CCOCC1)NC2=CC=CC(C3=C4C(C5=CC=C(CN6CCN(CCOC)CC6)C=C5)=NN3)=C2C4=O

Molecular Formula

C29H35N7O4

Molecular Weight

545.63

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]Cirstea D, et al. Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27 (12) :2366-75.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 1

Isoform

CDK1; CDK2; CDK3; CDK4; CDK5; CDK6; CDK7; CDK9; GSK-3β; JAK2; MEK1

Citation 01

Cancers (Basel) . 2022 Mar 19;14 (6) :1575.|Science. 2017 Dec 1;358 (6367) :eaan4368.|University of Washington. 2025.

Available Sizes

Curated Selection

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