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			96-Well Plate

数量	产品目录编号	订购说明	数量 / 包装	公开价
	48-602MAG	Buffer Detection Kit for Magnetic Beads	1 Kit

526561 Sigma-AldrichPI 3-K/mTOR Inhibitor III, PKI-179 - CAS 1197160-28-3 - Calbiochem

The PI 3-K/mTOR Inhibitor III, PKI-179, also referenced under CAS 1197160-28-3, controls the biological activity of PI 3-K/mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
小册子
Data Sheet

同义词: 1-(4-(4-(3-Oxa-8-azabicyclo[3.2.1]octan-8-yl)-6-morpholino-1,3,5-triazin-2-yl)-phenyl)-3-(pyridin-4-yl)urea, hydrate, N-(4-(4-(4-Morpholinyl)-6-(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazin-2-yl)phenyl)-Nʹ-4-pyridinylurea, hydrate, mTOR Inhibitor X, PI 3-K Inhibitor XVII

Recommended Products

概述

Replacement Information

重要规格表

CAS #	Empirical Formula
1197160-28-3	C₂₅H₂₈N₈O₃•H₂O

价格及供货情况

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Description
Overview	A cell-permeable triazinyl-phenyl-pyridinylurea compound that acts as a potent inhibitor against mTOR (IC₅₀ = 0.42 nM) and PI 3-K (IC₅₀ = 8, 24, 74, 77, 14, and 11 nM against isoform α, β, γ, δ, α E545K mutant, and α H1047R mutant, respectively) activities, exhibiting much reduced or little activity against a panel of 361 other kinases (IC₅₀ >50 µM), Cytochrome CYP isoforms, or hERG. It is reported to be orally available in mouse, rat, monkey, and dog species, and effectively suppress cancer growth both in cultures in vitro (IC₅₀ = 22 and 29 nM, respectively, against MDA361 and PC3mm2) and in mice in vivo (by 30% of control MDA361 tumor size on day 42; 50 mg/kg/day p.o.) via apoptosis induction as a result of Akt/mTOR pathway inhibition.
Catalogue Number	526561
Brand Family	Calbiochem®
Synonyms	1-(4-(4-(3-Oxa-8-azabicyclo[3.2.1]octan-8-yl)-6-morpholino-1,3,5-triazin-2-yl)-phenyl)-3-(pyridin-4-yl)urea, hydrate, N-(4-(4-(4-Morpholinyl)-6-(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazin-2-yl)phenyl)-Nʹ-4-pyridinylurea, hydrate, mTOR Inhibitor X, PI 3-K Inhibitor XVII

References
References	Venkatesan, A.M., et al. 2010. Bioorg. Med. Chem. Lett. 20, 5869. Chen, Z., et al. 2010. J. Org. Chem. 75, 1643.

Product Information
CAS number	1197160-28-3
Form	White solid
Hill Formula	C₂₅H₂₈N₈O₃•H₂O
Chemical formula	C₂₅H₂₈N₈O₃•H₂O
Hygroscopic	Hygroscopic
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Purity	≥98% by HPLC

Physicochemical Information

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Regulatory Review
Storage	+2°C to +8°C
Protect from Light	Protect from light
Hygroscopic	Hygroscopic
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
526561-5MGCN	04055977270358

Documentation

PI 3-K/mTOR Inhibitor III, PKI-179 - CAS 1197160-28-3 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

PI 3-K/mTOR Inhibitor III, PKI-179 - CAS 1197160-28-3 - Calbiochem 分析证书

标题	批号
526561	输入批号

参考

参考信息概述
Venkatesan, A.M., et al. 2010. Bioorg. Med. Chem. Lett. 20, 5869. Chen, Z., et al. 2010. J. Org. Chem. 75, 1643.

小册子

标题
New Products: Volume 3, 2012

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	08-October-2012 JSW
Synonyms	1-(4-(4-(3-Oxa-8-azabicyclo[3.2.1]octan-8-yl)-6-morpholino-1,3,5-triazin-2-yl)-phenyl)-3-(pyridin-4-yl)urea, hydrate, N-(4-(4-(4-Morpholinyl)-6-(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazin-2-yl)phenyl)-Nʹ-4-pyridinylurea, hydrate, mTOR Inhibitor X, PI 3-K Inhibitor XVII
Description	A cell-permeable triazinyl-phenyl-pyridinylurea compound that acts as a potent inhibitor against mTOR and PI 3-K activities (IC₅₀ = 0.42 nM against mTOR; IC₅₀ = 8, 24, 74, 77, 14, and 11 nM against PI 3-K isoform α, β, γ, δ, α E545K mutant, and α H1047R mutant, respectively), exhibiting much reduced potency against Cytochrome CYP 2C8 (IC₅₀ = 3 µM) and little or no activity toward 7 other Cytochrome CYP isoforms, hERG (IC₅₀ >30 µM) and a panel of 361 other kinases (IC₅₀ >50 µM). It is reported to be orally available in mouse, rat, monkey, and dog (bioavailability = 98%, 46%, 38%, and 61%, respectively; 10 mg/kg), and effectively suppress cancer growth both in cultures in vitro (IC₅₀ = 22 and 29 nM, respectively, against MDA361 and PC3mm2) and in mice in vivo (40% and 30% of control MDA361 tumor size on day 42, respectively, via daily p.o. dosage of 10 mg/kg and 50 mg/kg) via apoptosis induction as a result of Akt/mTOR pathway inhibition. Although liver microsome stability data indicate a much faster compound metabolism in human (t_1/2> = 14 min) and monkey than in mouse, rat (t_1/2> >30 min), and dog, the major metabolite remains biologically potent against kinase targets (IC₅₀ =0.8, 4, and 33 nM against mTOR, PI 3-Kα, and PI 3-γ, respectively) and cancer cell proliferation (IC₅₀ = 32 and 80 nM, respectively, against MDA361 and PC3mm2).
Form	White solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1197160-28-3
Chemical formula	C₂₅H₂₈N₈O₃•H₂O
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (50 mg/ml)
Storage	Protect from light +2°C to +8°C Hygroscopic
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Regulatory Review
References	Venkatesan, A.M., et al. 2010. Bioorg. Med. Chem. Lett. 20, 5869. Chen, Z., et al. 2010. J. Org. Chem. 75, 1643.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > mTOR Inhibitors

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