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Chemical Structure : CRT0066101
CAS No.: 1883545-60-5
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $248 | In stock | |
| 50 mg | $428 | In stock | |
| 100 mg | $728 | In stock | |
| 250 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 411.33 | |
| Formula | C18H22N6O.2HCl | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride |
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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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