NVS PAK1 1

Pricing Availability Delivery Time Qty
Cat.No. 6132 - NVS PAK1 1 | C23H25ClF3N5O | CAS No. 1783816-74-9
Description: Potent and selective PAK1 inhibitor
Chemical Name: (3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective PAK1 inhibitor (IC50 = 5 nM). Selective for PAK1 over PAK2 and a panel of 442 kinases. Inhibits autophosphorylation of PAK1 in KRAS-mutated pancreatic cancer cell lines.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the NVS-PAK1-1 probe summary on the SGC website.

Technical Data

M. Wt 479.93
Formula C23H25ClF3N5O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1783816-74-9
Smiles FC(F)CN(C(C=CC(F)=C1)=C1N=C2N[C@H]3CCN(C(NC(C)C)=O)C3)C4=C2C=C(Cl)C=C4

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
1eq. HCl 47.99 100
DMSO 47.99 100
ethanol 47.99 100

Preparing Stock Solutions

The following data is based on the product molecular weight 479.93. 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 2.08 mL 10.42 mL 20.84 mL
5 mM 0.42 mL 2.08 mL 4.17 mL
10 mM 0.21 mL 1.04 mL 2.08 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Karpov et al (2015) Optimization of a dibenzodiazepine hit to a potent and selective allosteric PAK1 inhibitor. ACS Med.Chem.Lett. 6 776 PMID: 6191365


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Keywords: NVS PAK1 1, supplier, NVSPAK11, P21-activated, kinases, PAK1, inhibitors, inhibits, potent, selective, P21-activated, Kinases, P21-activated, Kinases, Tocris Bioscience

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