WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H407867
CAS#: 1609452-30-3 (HCl)
Description: 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.
Hodoodo Cat#: H407867
Name: SEL120-34A HCl
CAS#: 1609452-30-3 (HCl)
Chemical Formula: C15H19Br2ClN4
Exact Mass: 0.00
Molecular Weight: 450.603
Elemental Analysis: C, 39.98; H, 4.25; Br, 35.47; Cl, 7.87; N, 12.43
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.
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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: | |
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| 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.
