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PKI-179 hydrochloride - 98%, high purity , CAS No.1463510-35-1

COA

Grade & Purity:

≥98%

Cas Number: 1463510-35-1
Molecular Weight: 525.00
PubChem CID: 137699924

In stock

Item Number

P648235

Grouped product items
SKU	Size	Availability	Price
P648235-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$250.90
P648235-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$400.90
P648235-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$800.90
P648235-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,280.90

View related series

mTOR (145) PI3K (243) PI3K/Akt/mTOR (765)

Basic Description

Specifications & Purity	≥98%
Biochemical and Physiological Mechanisms	PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC 50 s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α , PI3K-β , PI3K-γ , PI3K-δ and mTOR , respectively. PKI-179 hydrochloride also exhibits activity over E545K and
Storage Temp	Store at 2-8°C,Desiccated
Shipped In	Wet ice This product requires cold chain shipping. Ground and other economy services are not available.
Product Description	PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC 50 s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α , PI3K-β , PI3K-γ , PI3K-δ and mTOR , respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R , with IC 50 s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo In Vitro PKI-179 inhibits the cell proliferation, with IC 50 s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively. PKI-179 shows inhibitory activity against a panel of 361 other kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC 50 =3 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PKI-179 (5-50 mg/kg; p.o. once daily for 40 days) inhibits the tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors . PKI-179 (50 mg/kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts . PKI-179 exhibits good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice bearing MDA-361 human breast cancer tumors Dosage: 5, 10, 25, 50 mg/kg Administration: I.p. every 3 days for 4 weeks Result: Exhibited pronounced tumor growth arrest when dosed above 10 mg/kg. No significant weight loss of tested animals was observed for all different dosages. Form:Solid IC50& Target:mTOR 0.42 nM (IC 50 ) PI3Kα 8 nM (IC 50 ) PI3Kβ 24 nM (IC 50 ) PI3Kγ 74 nM (IC 50 ) PI3Kδ 77 nM (IC 50 ) E545K 14 nM (IC 50 ) H1047R 77 nM (IC 50 )

Names and Identifiers

IUPAC Name	1-[4-[4-morpholin-4-yl-6-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)-1,3,5-triazin-2-yl]phenyl]-3-pyridin-4-ylurea;hydrochloride
INCHI	InChI=1S/C25H28N8O3.ClH/c34-25(28-19-7-9-26-10-8-19)27-18-3-1-17(2-4-18)22-29-23(32-11-13-35-14-12-32)31-24(30-22)33-20-5-6-21(33)16-36-15-20;/h1-4,7-10,20-21H,5-6,11-16H2,(H2,26,27,28,34);1H
InChIKey	JNMURGIZAFELTR-UHFFFAOYSA-N
Smiles	C1CC2COCC1N2C3=NC(=NC(=N3)N4CCOCC4)C5=CC=C(C=C5)NC(=O)NC6=CC=NC=C6.Cl
PubChem CID	137699924
Molecular Weight	525.00

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