THAL SNS 032

Tocris Bioscience | Catalog # 6532

Potent and selective Cdk9 Degrader (PROTAC®)
Tocris Bioscience
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Key Product Details

Description

Potent and selective Cdk9 Degrader (PROTAC®)

Product Description

THAL SNS 032 is a degrader (PROTAC®) comprising the cyclin-dependent kinase inhibitor SNS 032 (Cat. No. 4075) conjugated to the cereblon E3 ligase ligand, thalidomide (Cat. No. 0652). Potent, selective and cereblon-dependent degrader of Cdk9 (EC50 = 4 nM). Displays >15-fold selectivity for Cdk9 over other CDKs (EC50 values are 62, 171 and 398 nM for Cdk2, Cdk1 and Cdk7, respectively). Induces complete degradation of Cdk9 at 250 nM in MOLT4 cells. Inhibits proliferation of leukemia cell lines.

Cdk9 antibodies validated for Western Blot also available: Catalog # NBP2-15848 and NBP3-15345.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Scientific Data Images for THAL SNS 032

Application of THAL SNS 032 in MOLT-4 cells

Application of THAL SNS 032 in MOLT-4 cells.

Western Blot data showing knockdown of both CDK9 isoforms after THAL SNS 032 treatment of MOLT-4 cells (4 h incubation). Protein quantification (relative to DMSO-only control) is shown beneath the corresponding lane. Cdk9 primary antibody is used at 1:1000 dilution. Secondary is Anti-Rabbit HAF008, 1:1000, R&D Systems. GAPDH primary antibody is R&D Systems AF5718 used at 5μg/mL. Secondary is Anti-Goat HAF017, 1:1000, R&D Systems.Data courtesy of Jeff Cooper, Bio-Techne.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Product Specifications for THAL SNS 032

Molecular Weight

869.02

Formula

C40H52N8O10S2

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

N-(5-(((5-(tert-Butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxo-6,9,12-trioxa-3-azatetradecyl)piperidine-4-carboxamide

CAS Number

2139287-33-3

PubChem ID

131801483

InChI Key

BXDZOYLPNAIDOC-UHFFFAOYSA-N

SMILES

CC(C)(C1=CN=C(O1)CSC2=CN=C(S2)NC(C3CCN(CC3)CC(NCCOCCOCCOCCNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O)=O)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 86.9 100

Preparing Stock Solutions for THAL SNS 032

The following data is based on the product molecular weight 869.02.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.75 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.30 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 4 publications citing the usage of this product.

Product Documents for THAL SNS 032

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for THAL SNS 032

For research use only

Related Research Areas

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