HS-173 1276110-06-5

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Molecular Weight: 422.46 HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.

HS-173 shows potent antiproliferative effects in T47D, SK-BR3, and MCF7 cells with IC50 of 0.6, 1.5, and 7.8 μM, respectively. HS-173 causes complete suppression of the PI3K pathway in cancer cell
lines (Hep3B and SkBr3). Moreover, HS-173 induces cell Apoptosis by
affecting cell-cycle distribution and activating caspases, and block
VEGF-induced Angiogenesis in vitro. Combined treatment with Sorafenib and HS-173 has a synergistic anti-cancer effect on pancreatic cancer cells.

HS-173 diminishes blood vessel formation in mice. HS-173 markedly attenuates the development of liver fibrosis by blocking PI3K/Akt signaling in vivo.

PI3-Kinase assay

The PI3K assay is performed using the Kinase-Glo Max luminescent kinase assay kit which quantifies the amount of ADP produced by the PI3K reaction. In brief, an active PI3K (100 ng) is preincubated with compound for 5 min in kinase reaction buffer (25 mM MOPS [pH 7.0], 5 mM MgCl2, and 1 mM EGTA) and 10 μg l-α-phosphatidylinositol (PI). Before addition of PI, it is sonicated with sonication buffer (25 mM MOPS [pH 7.0], 1 mM EGTA) in water for 20 min for allowing miscelle formation. Then reaction is started by the addition of 10 μM ATP and ran for 180 min. To terminate kinase reaction, same volume of Kinase-Glo Max buffer is added. After 10 min, the plates are then read on a GloMax plate reader for luminescence detection.

Cell Assay: [1]

Cell lines	T47D, SK-BR3, MCF7 cells
Concentrations	~50 μM
Incubation Time	48 hours
Method	Cell viability is performed by a MTT assay. Briefly, T47D cells are plated in 96-well plates for 24 h. Then, the medium is removed and cells were treated with either DMSO as a control or various concentrations of Inhibitors. The final concentration of DMSO in the medium was ≤0.1% (v/v). After the cells are incubated for 48 h, 20 μL MTT solution (5 mg/mL) is added to each well for another 4 h at 37 °C. The formazan crystals that formed are dissolved in DMSO (100 μL/well) by constant shaking for 5 min. The plate is then read on a microplate reader at 540 nm. Three replicate wells are used for each analysis. The median inhibitory concentration (IC50, defined as the drug concentration at which cell growth is inhibited by 50%) is assessed from the dose−response curves. To assess the effect of compounds on cell proliferation, T47D cells are cultured with compound (0.1−100 μM) for 48 h before MTT analysis.

Animal Study: [4]

Animal Models	Male BALB/c mice with CCl4-induced liver fibrosis
Formulation	Dissolved in DMSO, and then mixture (DMSO:PEG400:D.W. = 1:5:4).
Dosages	~20 mg/kg
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)	422.46
Formula	C21H18N4O4S
CAS No.	1276110-06-5

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

Solubility (25°C) *	In vitro	DMSO	84 mg/mL heating (198.83 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
* <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	ethyl 6-(5-(phenylsulfonamido)pyridin-3-yl)imidazo[1,2-a]pyridine-3-carboxylate

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Product Categories : PI3K/Akt/mTOR > PI3K Inhibitor