THAL SNS 032

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Cat.No. 6532 - THAL SNS 032 | C40H52N8O10S2 | CAS No. 2139287-33-3
Description: Potent and selective CDK9 degrading PROTAC
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
Purity: ≥98% (HPLC)
Datasheet
Citations
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Literature

Biological Activity

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.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data

M. Wt 869.02
Formula C40H52N8O10S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2139287-33-3
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 869.02. Batch specific molecular weights may vary from batch to batch due to solvent 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 5.75 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

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References

References are publications that support the biological activity of the product.

Olson et al (2018) Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat.Chem.Biol. 14 163 PMID: 29251720


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Keywords: THAL SNS 032, THAL SNS 032 supplier, THALSNS032, potent, selective, CDK9, degraders, degrades, PROTAC, proteolysis, targeting, chimera, PROTACs, Cyclin-dependent, Kinase, 6532, Tocris Bioscience

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