RGB-286638 | CDK inhibitor | Probechem Biochemicals

Chemical Structure : RGB-286638

CAS No.: 784210-87-3

RGB-286638 (RGB286638)

Catalog No.: PC-21089Not For Human Use, Lab Use Only.

RGB-286638 is a small-molecule multi-targeted cyclin-dependent kinase (CDK) inhibitor with IC50 of 1-5 nM for cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5.

Packing	Price	Stock
5 mg	$98	In stock
10 mg	$148	In stock
25 mg	$258	In stock
50 mg	$428	In stock
100 mg		Get quote

Get Quotation Now

* Please select Quantity before adding items.

or Bulk Inquiry

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Biological Activity

RGB-286638 is a small-molecule multi-targeted cyclin-dependent kinase (CDK) inhibitor with IC50 of 1-5 nM for cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5.
RGB-286638 is less potent against cyclin H-CDK7 and cyclin D3-CDK6.
RGB-286638 also inhibits several tyrosine and serine/threonine non-CDK enzymes with IC50 of 1-50 nM, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1.
RGB-286638 potently inhibits cell growth of human p53-wt (MM.1S, MM.1R, and H929) and p53-mutant (U266, OPM1, and RPMI) MM cells with EC50 of 20-70 nM.
RGB-286638 (50nM) reduces the phosphorylation of Rb at S807/811 in MM.1S and MM.1R cells, but has no effects on p-Rb S780.
RGB-286638 induces cytotoxicity in p53 knockdown MM.1S, exhibits anti-MM activity in vivo.

Physicochemical Properties

M.Wt	618.56
Formula	C29H37Cl2N7O4
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-[1,4-Dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N′-4-morpholinylurea hydrochloride (1:2)

References

1. Cirstea D, et al. Leukemia. 2013 Dec;27(12):2366-75.

2. van der Biessen DA, et al. Clin Cancer Res. 2014 Sep 15;20(18):4776-83.

RGB-286638 (RGB286638)

Biological Activity

Physicochemical Properties

References

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

Get Quote

* Indicates a Required FieldYour information is safe with us.