HO-3867 1172133-28-6

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Molecular Weight:

464.55 HO-3867, an analog of curcumin, is a selective STAT3 inhibitor.


Biological Activity


HO-3867 produces significant cytotoxicity in A2780 and other tested
ovarian cancer cell lines, with less toxic to noncancerous ovarian
surface epithelial cells. HO-3867 induces G(2)-M Cell Cycle arrest in
A2780 cells and promotes Apoptosis by caspase-8 and caspase-3
activation. HO-3867 blocks the JAK/STAT3 pathway in human ovarian cancer
cell lines.


HO-3867 (100 ppm p.o.) inhibits the growth of ovarian cancer xenograft
tumor in mice without any apparent signs of toxicity, and also results
in inhibition of pSTAT3 as well as downregulation of the STAT3-targeting
Proteins. HO-3867 sensitizes cisplatin-resistant ovarian carcinoma
through STAT3 inhibition. HO-3867 (100 ppm p.o.) also attenuates
left-heart-failure-induced pulmonary hypertension by decreasing
oxidative stress and increasing PTEN expression in the lung of rats.


Protocol(Only for Reference)


Cell Assay: [1]

Cell lines	A2780 (A2780R), PA-1, SKOV3, OV4, and OVCAR3 cells; human ovarian surface epithelial cell
Concentrations	~20 μM
Incubation Time	24 hours
Method	Cell viability is determined by a colorimetric assay using MTT. In the mitochondria of living cells, yellow MTT undergoes a reductive conversion to formazan, producing a purple color. Cells, grown to ~80% confluence in 75-mm flasks, are trypsinized, counted, seeded in 96-well plates with an average population of 7,000 cells/well, incubated overnight, and then treated with HO-3867 for 24 h. All experiments are done using 8 replicates and repeated at least three times.

Animal Study: [1]

Animal Models	Mice bearing ovarian cancer A2780 tumor xenografts
Formulation
Dosages	~100 ppm
Administration	p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	464.55
Formula	C28H30F2N2O2
CAS No.	1172133-28-6

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	N/A

Solubility (25°C) *	In vitro	DMSO	13 mg/mL heating (27.98 mM)
		Water	<1 mg/mL (
		Ethanol	6 mg/mL heating (12.91 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	1-[(2,5-dihydro-1-hydroxy-2,2,5,5-tetramethyl-1H-pyrrol-3-yl)methyl]-3,5-bis[(4-fluorophenyl)methylene]-(3E,5E)-4-piperidinone

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Product Categories : JAK/STAT > STAT inhibitor