CRT 0066101

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Cat.No. 4975 - CRT 0066101 | C18H22N6O.2HCl | CAS No. 1883545-60-5
Description: Potent protein kinase D (PKD) inhibitor
Chemical Name: 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews (1)
Literature

Biological Activity

Potent inhibitor of protein kinase D (PKD); inhibits all PKD isoforms (IC50 values are 1, 2 and 2.5 nM for PKD1, PKD3 and PKD2 respectively). Exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα, MEK, ERK, c-Raf and c-Src. Reduces proliferation and cell viability of pancreatic cancer cells expressing moderate levels of endogenous PKD1/2. Orally bioavailable.

Technical Data

M. Wt 411.33
Formula C18H22N6O.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1883545-60-5
PubChem ID 69074905
InChI Key CXYCRYGNFKDPRH-FMOMHUKBSA-N
Smiles OC1=C(C3=NC(NC[C@@H](CC)N)=CC=N3)C=C(C2=CN(C)N=C2)C=C1.Cl.Cl

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
water 41.13 100
DMSO 8.23 20

Preparing Stock Solutions

The following data is based on the product molecular weight 411.33. 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 2.43 mL 12.16 mL 24.31 mL
5 mM 0.49 mL 2.43 mL 4.86 mL
10 mM 0.24 mL 1.22 mL 2.43 mL
50 mM 0.05 mL 0.24 mL 0.49 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

Harikumar et al (2010) A novel small molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo. Mol.Cancer Ther. 9 1136 PMID: 20442301

Ni et al (2013) PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors. PLoS ONE 9 e73149 PMID: 24039875


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Keywords: CRT 0066101, CRT 0066101 supplier, CRT0066101, potent, pan, protein, kinase, D, PKD, PKD1, PKD2, PKD3, inhibits, inhibitors, Protein, Kinase, 4975, Tocris Bioscience

2 Citations for CRT 0066101

Citations are publications that use Tocris products. Selected citations for CRT 0066101 include:

Jensen et al (2016) Protein kinase D and Gβγ subunits mediate agonist-evoked translocation of protease-activated receptor-2 from the Golgi apparatus to the plasma membrane. J.Biol.Chem. 291 11285 PMID: 27030010

Liou et al (2015) Protein kinase D1 drives pancreatic acinar cell reprogramming and progression to intraepithelial neoplasia. Sci Rep 6 6200 PMID: 25698580


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Reviews for CRT 0066101

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Very potent PKD inhibitor
By Anonymous on 11/06/2017
Assay Type: In Vivo
Species: Mouse

The product was used per os on mice for an invivo study.

the CRT0066101 PKD inhibitor can be dissolved in normal saline or DMSO easily (depends of the concentration)


Literature in this Area

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Cancer

Cancer Research Product Guide

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Kinases Product Listing

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