CZC-8004 (CZC-00008004) is an aminopyrimidine and a pan-kinase inhibitor. CZC-8004 can bind to a series of tyrosine kinases like EGFR and VEGFR2, with IC50s of 650 and 437 nM respectively.

Physicochemical Properties

Molecular Formula	C17H16FN5
Molecular Weight	309.3408
Exact Mass	309.138
CAS #	916603-07-1
PubChem CID	15980598
Appearance	White to off-white solid powder
Density	1.3±0.1 g/cm3
Boiling Point	514.1±60.0 °C at 760 mmHg
Flash Point	264.7±32.9 °C
Vapour Pressure	0.0±1.3 mmHg at 25°C
Index of Refraction	1.699
LogP	2.27
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	5
Heavy Atom Count	23
Complexity	342
Defined Atom Stereocenter Count	0
InChi Key	UKOHFWNBTUJMMN-UHFFFAOYSA-N
InChi Code	InChI=1S/C17H16FN5/c18-15-11-20-17(22-14-8-6-12(10-19)7-9-14)23-16(15)21-13-4-2-1-3-5-13/h1-9,11H,10,19H2,(H2,20,21,22,23)
Chemical Name	2-N-[4-(aminomethyl)phenyl]-5-fluoro-4-N-phenylpyrimidine-2,4-diamine
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References	CZC-8004 is a pan-kinase inhibitor, with low micromolar IC50 for tyrosine kinase. [2]. Bantscheff M, et al. Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors. Nat Biotechnol. 2007 Sep;25(9):1035-44.
Additional Infomation	CZC8004 is an aminopyrimidine and an organofluorine compound. It has a role as a protein kinase inhibitor.

Solubility Data

Solubility (In Vitro)

DMSO : ~77.5 mg/mL (~250.53 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.58 mg/mL (8.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.58 mg/mL (8.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.58 mg/mL (8.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.2327 mL	16.1634 mL	32.3269 mL
	5 mM	0.6465 mL	3.2327 mL	6.4654 mL
	10 mM	0.3233 mL	1.6163 mL	3.2327 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.