SEL120-34A HCl | CAS#1609452-30-3 | 1609522-33-9 | CDK8 inhibitor

MedKoo Cat#: 407867 | Name: SEL120-34A HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

SEL120-34A is a potent and selective CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. EL120-34A inhibits phosphorylation of STAT1 S727 and STAT5 S726 in cancer cells in vitro. Consistently, regulation of STATs- and NUP98-HOXA9- dependent transcription has been observed as a dominant mechanism of action in vivo.

Chemical Structure

SEL120-34A HCl

CAS#1609452-30-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 407867

Name: SEL120-34A HCl

CAS#: 1609452-30-3 (HCl)

Chemical Formula: C15H19Br2ClN4

Exact Mass: 0.0000

Molecular Weight: 450.60

Elemental Analysis: C, 39.98; H, 4.25; Br, 35.47; Cl, 7.87; N, 12.43

Price and Availability

Size	Price	Availability
5mg	USD 90.00	Ready to ship
10mg	USD 150.00	Ready to Ship
25mg	USD 250.00	Ready to Ship
50mg	USD 450.00	Ready to Ship
100mg	USD 750.00	Ready to Ship
200mg	USD 1,350.00	Ready to Ship

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Related CAS #

1609522-33-9 (free base) 1609452-30-3 (HCl)

Synonym

SEL120-34A; SEL 120-34A; SEL-120-34A; SEL12034A; SEL 12034A; SEL-12034A.

IUPAC/Chemical Name

7,8-Dibromo-9-methyl-2-piperazin-1-yl-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline Hydrochloride

InChi Key

GQXLWUCQESKBSC-UHFFFAOYSA-N

InChi Code

InChI=1S/C15H18Br2N4.ClH/c1-9-11(16)12(17)10-3-2-6-21-14(10)13(9)19-15(21)20-7-4-18-5-8-20;/h18H,2-8H2,1H3;1H

SMILES Code

CC1=C(Br)C(Br)=C2CCCN3C2=C1N=C3N4CCNCC4.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Treatment with the compound resulted in a differential efficacy on AML cells with elevated STAT5 S726 levels and stem cell characteristics. In contrast, resistant cells were negative for activated STAT5 and revealed lineage commitment. In vivo efficacy in xenotransplanted AML models correlated with significant repression of STAT5 S726. Favorable pharmacokinetics, confirmed safety and in vivo efficacy provide a rationale for the further clinical development of SEL120-34A as a personalized therapeutic approach in AML.

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#Y22X11M23

QC Data

View QC data: current batch, Lot#Y22X11M23

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

In vitro activity:

Collectively, these results suggest that SEL120-34A inhibits IFN-dependent gene expression, however the effects on these genes are modest and transient, indicating that CDK8 is not a major driver of STAT-dependent transcription in IFN-stimulated cancer cells in vitro. Reference: Oncotarget. 2017 May 16;8(20):33779-33795. https://pubmed.ncbi.nlm.nih.gov/28422713/

In vivo activity:

Next, this study assessed in vivo activity of SEL120-34A in xenografted KG-1 and MV4-11 AML tumors grown in SCID mice models. SEL120-34A treatment resulted in completely arrested growth of KG-1-derived tumors and a reduced volume of MV4-11 tumors, without appreciable loss in body weight (Figure 9A and 9B). Reference: Oncotarget. 2017 May 16;8(20):33779-33795. https://pubmed.ncbi.nlm.nih.gov/28422713/

	Solvent	mg/mL	mM
Solubility
	DMSO	31.8	70.46
	Water	90.0	199.73

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 450.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Rzymski T, Mikula M, Żyłkiewicz E, Dreas A, Wiklik K, Gołas A, Wójcik K, Masiejczyk M, Wróbel A, Dolata I, Kitlińska A, Statkiewicz M, Kuklinska U, Goryca K, Sapała Ł, Grochowska A, Cabaj A, Szajewska-Skuta M, Gabor-Worwa E, Kucwaj K, Białas A, Radzimierski A, Combik M, Woyciechowski J, Mikulski M, Windak R, Ostrowski J, Brzózka K. SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. Oncotarget. 2017 May 16;8(20):33779-33795. doi: 10.18632/oncotarget.16810. PMID: 28422713; PMCID: PMC5464911.

In vitro protocol:

In vivo protocol:

1: Rzymski T, Mikula M, Żyłkiewicz E, Dreas A, Wiklik K, Gołas A, Wójcik K, Masiejczyk M, Wróbel A, Dolata I, Kitlińska A, Statkiewicz M, Kuklinska U, Goryca K, Sapała Ł, Grochowska A, Cabaj A, Szajewska-Skuta M, Gabor-Worwa E, Kucwaj K, Białas A, Radzimierski A, Combik M, Woyciechowski J, Mikulski M, Windak R, Ostrowski J, Brzózka K. SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. Oncotarget. 2017 May 16;8(20):33779-33795. doi: 10.18632/oncotarget.16810. PubMed PMID: 28422713; PubMed Central PMCID: PMC5464911. 2: Kuang, Y., Golan, O., Preusse, K., Cain, B., Christensen, C. J., Salomone, J., ... & Gebelein, B. (2020). Enhancer architecture sensitizes cell specific responses to Notch gene dose via a bind and discard mechanism. Elife, 9, e53659.