PHT-427 1191951-57-1

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Molecular Weight: 409.61 PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 μM and 5.2 μM, respectively.

PH-427 is a pleckstrin homology domain inhibitor to Akt/PDPK1. PH-427
significantly reduces phospho-Ser241-PDPK1 phospho-Thr308-Akt in PC-3
prostate cancer cells at 10 μM, which shows that PHT-427 could inhibit
both Akt and PDPK1. PHT-427 also inhibits translocation of the Akt and
PDPK1 PH domains in plasma membrane. PHT-427 induces
Apoptosis and inhibits AKT phosphorylation with IC50 of 8.6 μM (in
BxPC-3 cells), which mainly on its Ser473 residue and less strongly on
Thr308 residue without affecting total Akt protein expression. PHT-427
also shows antiproliferation in Panc-1 cells with IC50 of 65 μM.





PHT-427 shows great antitumor activity in BxPC-3 pancreatic, MCF-7
breast and A-549 NSCL cancer xenografts. PHT-427 gives up to an 80%
inhibition of tumor growth in BxPC-3 at doses of 125 to 250 mg/kg.

Surface plasmon resonance (SPR) spectroscopy binding assays

All interaction analyses are performed with a Biacore 2000, Biacore 2000 Control Software v3.2, and BIAevaluation v4.1 analysis software. The PH domain GST-fusion Proteins (Akt1, IRS1, and PDK1) are immobilized on a CM5 Sensorchip using Biacore's Amine Coupling Kit to a level of 10,000 Response units (RUs). Small molecule analytes at concentrations ranging from 0.1 to 10 × the predicted KD are injected at a high flow rate (30μL/min). DMSO concentrations in all samples and running buffer are 1% (v/v) or less.

Cell Assay: [2]

Cell lines	Panc-1 cells
Concentrations	1-50 μM
Incubation Time
Method	Cell growth inhibition is determined using a micro-cytoxicity assay. Cells are plated in 96-well micro-cytoxicity at 5-10 × 103 cells per well (depending on cell doubling time) and grown for 7 days. PHT-427 dissolved in DMSO is added directly to the media, at various concentrations ranging from 1 to 50 μM. The endpoint is spectrophotometric determination of the protein content of each well using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. A concentration-response relationship at two or more concentration levels is used to obtain an IC50 for PHT-427.

Animal Study: [1]

Animal Models	BxPC-3, Panc-1, MiaPaCa-2, PC-3, SKOV-3, A-549 or MCF-7 cells are injected subcutaneously into the flanks of female scid mice.
Formulation	40 to 50 mg/mL in sesame seed oil
Dosages	125-250 mg/kg
Administration	Oral administration
Solubility	5% DMSO/95% Corn oil, 5 mg/mL
* 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.

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)	409.61
Formula	C20H31N3O2S2
CAS No.	1191951-57-1

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	CS-0223

Solubility (25°C) *	In vitro	DMSO	82 mg/mL (200.19 mM)
		Water	<1 mg/mL (
		Ethanol	60 mg/mL (146.48 mM)
	In vivo	5% DMSO/95% Corn oil	5 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	4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide

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Product Categories : PI3K/Akt/mTOR > Akt Inhibitor