CRT 0066101

Name: CRT 0066101
Brand: Tocris Bioscience
SKU: 4975
Rating: 5 (4 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 4975

(4)

Citations (41)

COA / SDS

Potent protein kinase D (PKD) inhibitor

Key Product Details

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)
Molecular Weight:	411.33

View Full Technical Details for CRT 0066101

Technical Data
Citations / Reviews (4)

Biological Activity for CRT 0066101

CRT 0066101 is a 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 for CRT 0066101

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 for CRT 0066101

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	41.13	100
	DMSO	8.23	20

Preparing Stock Solutions for CRT 0066101

The following data is based on the product molecular weight 411.33.

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	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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References for CRT 0066101

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

Ni PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors. PLoS ONE 2013 PMID: 24039875
Harikumar A novel small molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo. Mol.Cancer Ther. 2010 PMID: 20442301