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NVP 2

Cat. No. 6535 Submit a Review Datasheet / COA / SDS
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Cat.No. 6535 - NVP 2 | C27H37ClN6O2 | CAS No. 1263373-43-8
Description: Potent and selective ATP-competitive CDK9 inhibitor
Chemical Name: 4-[[[5'-Chloro-2'-[[trans-4-[[(1R)-2-methoxy-1-methylethyl]amino]cyclohexyl]amino][2,4'-bipyridin]-6-yl]amino]methyl]tetrahydro-2H-pyran-4-carbonitrile
Purity: ≥97% (HPLC)
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent and selective ATP-competitive CDK9 inhibitor (IC50 = 0.5 nM). Exhibits selectivity for CDK9 over a panel of 468 kinases, but inhibits DYRK1B (IC50 = 350 nM), displays <90% binding to CDK7 (IC50 >10 μM) and CDK13. Inhibits proliferation of MOLT4 cells in vitro. Induces apoptosis.

Technical Data

M. Wt 513.07
Formula C27H37ClN6O2
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 1263373-43-8
PubChem ID 66937006
InChI Key XWQVQSXLXAXOPJ-QNGMFEMESA-N
Smiles COC[C@H](N[C@H]1CC[C@H](NC2=CC(C3=NC(NCC4(C#N)CCOCC4)=CC=C3)=C(C=N2)Cl)CC1)C

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 51.31 100
ethanol 51.31 100

Preparing Stock Solutions

The following data is based on the product molecular weight 513.07. 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 1.95 mL 9.75 mL 19.49 mL
5 mM 0.39 mL 1.95 mL 3.9 mL
10 mM 0.19 mL 0.97 mL 1.95 mL
50 mM 0.04 mL 0.19 mL 0.39 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

Winter et al (2017) BET bromodomain proteins function as master transcription elongation factors independent of CDK9 recruitment. Mol.Cell 67 5 PMID: 28673542

If you know of a relevant reference for NVP 2, please let us know.

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