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CRT0066101

Chemical Structure : CRT0066101

CAS No.: 1883545-60-5

CRT0066101 (CRT-0066101;CRT 0066101)

Catalog No.: PC-60928Not For Human Use, Lab Use Only.

CRT0066101 (CRT-0066101) is a potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CRT0066101 (CRT-0066101) is a potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.
CRT0066101 shows selectivity against a panel of > 90 protein kinases including PKCα/PKBα/MEK/ERK/c-Raf/c-Src/c-Abl.
CRT0066101 reduces bromodeoxyuridine incorporation, increases apoptosis, blocks neurotensin-induced PKD1/2 activation and reduces neurotensin-induced, PKD-mediated Hsp27 phosphorylation, attenuated PKD1-mediated NF-kappaB activation in pancreatic cancer cells.
CRT0066101 potently blocks tumor growth in vivo.

Physicochemical Properties

M.Wt 411.33
Formula C18H22N6O.2HCl
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride

References

1. Harikumar KB, et al. Mol Cancer Ther. 2010 May;9(5):1136-46.

2. Thrower EC, et al. Am J Physiol Gastrointest Liver Physiol. 2011 Jan;300(1):G120-9.

3. Borges S, et al. Mol Cancer Ther. 2015 Jun;14(6):1306-16.

4. Coughlan KA, et al. J Biol Chem. 2016 Mar 11;291(11):5664-75.

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