ICCB280 is a potent C/EBPα inducer. ICCB280 has anti-leukemic properties like terminal differentiation, proliferation arrest and apoptosis, by activating C/EBPα and affecting its downstream targets (like C/EBPε, G-CSFR and c-Myc).

Physicochemical Properties

Molecular Formula	C₂₃H₁₈N₂O₄
Molecular Weight	386.40
Exact Mass	386.126
CAS #	2041072-41-5
Related CAS #	2041072-41-5
PubChem CID	135500267
Appearance	Solid
Density	1.3±0.1 g/cm3
Boiling Point	624.1±65.0 °C at 760 mmHg
Flash Point	331.2±34.3 °C
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.644
LogP	3.89
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	4
Heavy Atom Count	29
Complexity	649
Defined Atom Stereocenter Count	0
SMILES	O(C)C1C=CC=CC=1N1C(C2C=CC=CC=2N=C1/C=C/C1C=CC(=C(C=1)O)O)=O
InChi Key	OTKDKQJFWIGZLU-ACCUITESSA-N
InChi Code	InChI=1S/C23H18N2O4/c1-29-21-9-5-4-8-18(21)25-22(13-11-15-10-12-19(26)20(27)14-15)24-17-7-3-2-6-16(17)23(25)28/h2-14,26-27H,1H3/b13-11+
Chemical Name	2-[(E)-2-(3,4-dihydroxyphenyl)ethenyl]-3-(2-methoxyphenyl)quinazolin-4-one
Synonyms	ICCB-280; ICCB280; ICCB 280
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

Targets	C/EBPα
ln Vitro	ICCB280 (0.1-50 μM; 48 h) suppresses the HL-60 cell growth, with an IC50 of 8.6 μM[1]. ICCB280 (10 μM; 2-8 d)) elevates C/EBP expression (mRNA and protein) and modifies its target genes in HL-60 cells[1]. ICCB280 (10 μM; 7 d) causes granulocytic differentiation and subsequently apoptosis in HL-60 cells[1].
References	[1]. A Cell-Based High-Throughput Screening for Inducers of Myeloid Differentiation. J Biomol Screen. 2015 Oct;20(9):1150-9. [2]. Styryl Quinazolinones as Potential Inducers of Myeloid Differentiation via Upregulation of C/EBPα. Molecules. 2018 Aug 3;23(8):1938.

Solubility Data

Solubility (In Vitro)

DMSO: ~83.3 mg/mL (~215.7 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (5.38 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 20.8 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: ≥ 2.08 mg/mL (5.38 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 20.8 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.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.5880 mL	12.9400 mL	25.8799 mL
	5 mM	0.5176 mL	2.5880 mL	5.1760 mL
	10 mM	0.2588 mL	1.2940 mL	2.5880 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.