Avagacestat (BMS-708163)

製品コード：S1262 純度：99.63%

Avagacestat (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.

CAS No. 1146699-66-2

サイズ	価格(税別)	在庫状況
5mg	JPY 25500	国内在庫あり
10mg	JPY 48000	国内在庫あり
50mg	JPY 145500	国内在庫あり
1g	JPY 748500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

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現在のバッチを見る：純度： 99.63%

99.63

Avagacestat (BMS-708163)関連製品

関連ターゲット	gamma-secretase	もっと見る
関連製品	DAPT RO4929097 DBZ (Dibenzazepine) LY411575 MK-0752 Semagacestat (LY450139) Nirogacestat (PF-03084014) MDL-28170 L-685,458	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Protease Inhibitor Library Ubiquitination Compound Library	もっと見る

Secretase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
human IMR32 cell	Function assay	2 h	Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA, IC50=0.13 nM	23312944
human IMR32 cell	Function assay	2 h	Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA, IC50=1.5 nM	23312944
human H4 cells	Function assay		Inhibition of gamma secretase-mediated amyloid beta42 production in human H4 cells expressing human APP swedish mutant, IC50=0.225 μM	22420884
HEK293 cells	Function assay		Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis, IC50=1.2 nM	23312944
CHO cells	Function assay		Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA, ED50=1.2 nM	23713656
human 786-0 cell	Growth inhibition assay		Inhibition of human 786-0 cell growth in a cell viability assay, IC50=0.32173 μM	SANGER
human NCI-H810 cell	Growth inhibition assay		Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=0.42598 μM	SANGER
human IGR-1 cell	Growth inhibition assay		Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=1.04778 μM	SANGER
human SK-MEL-3 cell	Growth inhibition assay		Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=1.49922 μM	SANGER
human HT-1080 cell	Growth inhibition assay		Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=2.48764 μM	SANGER
human NCI-H23 cell	Growth inhibition assay		Inhibition of human NCI-H23 cell growth in a cell viability assay, IC50=3.9322 μM	SANGER
human Calu-6 cell	Growth inhibition assay		Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=4.96014 μM	SANGER
human CAPAN-1 cell	Growth inhibition assay		Inhibition of human CAPAN-1 cell growth in a cell viability assay, IC50=5.17886 μM	SANGER
human COLO-668 cell	Growth inhibition assay		Inhibition of human COLO-668 cell growth in a cell viability assay, IC50=5.40221 μM	SANGER
human TE-6 cell	Growth inhibition assay		Inhibition of human TE-6 cell growth in a cell viability assay, IC50=6.19082 μM	SANGER
human LCLC-97TM1 cell	Growth inhibition assay		Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=10.0886 μM	SANGER
human CAS-1 cell	Growth inhibition assay		Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=13.671 μM	SANGER
human RPMI-2650 cell	Growth inhibition assay		Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50=13.8124 μM	SANGER
human MDA-MB-157 cell	Growth inhibition assay		Inhibition of human MDA-MB-157 cell growth in a cell viability assay, IC50=14.2431 μM	SANGER
human KINGS-1 cell	Growth inhibition assay		Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50=14.3762 μM	SANGER
human BB49-HNC cell	Growth inhibition assay		Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=14.4138 μM	SANGER
human SK-UT-1 cell	Growth inhibition assay		Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=14.6882 μM	SANGER
human EW-11 cell	Growth inhibition assay		Inhibition of human EW-11 cell growth in a cell viability assay, IC50=14.8832 μM	SANGER
human D-502MG cell	Growth inhibition assay		Inhibition of human D-502MG cell growth in a cell viability assay, IC50=14.9034 μM	SANGER
human MMAC-SF cell	Growth inhibition assay		Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50=15.0833 μM	SANGER
human NCI-H1648 cell	Growth inhibition assay		Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=15.778 μM	SANGER
human NCI-H292 cell	Growth inhibition assay		Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50=15.8806 μM	SANGER
human NMC-G1 cell	Growth inhibition assay		Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=16.6293 μM	SANGER
human SAS cell	Growth inhibition assay		Inhibition of human SAS cell growth in a cell viability assay, IC50=17.7812 μM	SANGER
human HCT-116 cell	Growth inhibition assay		Inhibition of human HCT-116 cell growth in a cell viability assay, IC50=18.7965 μM	SANGER
human SBC-5 cell	Growth inhibition assay		Inhibition of human SBC-5 cell growth in a cell viability assay, IC50=19.03 μM	SANGER
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

特性

Appears to be more “notch sparing” than semagacestat (LY450139).

Targets

Aβ42 ^[1] (in H4-8Sw cells)	Aβ40 ^[1] (in H4-8Sw cells)
0.27 nM	0.3 nM

In Vitro
In vitro	BMS-708163 exhibits weaker selectivity for inhibition of Notch processing with 193-fold IC50 value. ^[1]

In Vivo
In Vivo	Oral administration of BMS-708163 significantly reduces Aβ40 levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs. BMS-708163 has no dose-limiting effects in dogs (3 mg/kg during 6 months), with a high brain to plasma ratio (2.4). ^[1]
動物実験	動物モデル	Female Harlan Sprague-Dawley rats or ATM-405-142K9 with 7- 10 month old Na?ve, grade II beagles
	投与量	10 mg/kg (rats) or 2.5 mg/kg (dogs)
	投与経路	Dosed daily by oral gavage

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT01002079	Completed	Alzheimer Disease	Bristol-Myers Squibb\|PRA Health Sciences	August 2010	Phase 1
NCT01057030	Completed	Alzheimer Disease	Bristol-Myers Squibb	March 2010	Phase 1
NCT01042314	Completed	Alzheimer Disease	Bristol-Myers Squibb	January 2010	Phase 1
NCT01039194	Completed	Alzheimer Disease	Bristol-Myers Squibb	January 2010	Phase 1
NCT00979316	Completed	Alzheimer Disease	Bristol-Myers Squibb	September 2009	Phase 1
NCT00890890	Terminated	Alzheimer''s Disease	Bristol-Myers Squibb	May 2009	Phase 2

参考
[1] Gillman KW, et al. Med Chem Lett, 2010, 1 (3), 120–124.

参考

[1] Gillman KW, et al. Med Chem Lett, 2010, 1 (3), 120–124.

化学情報

分子量	520.88	化学式	C₂₀H₁₇ClF₄N₄O₄S
CAS No.	1146699-66-2	SDF	Download Avagacestat (BMS-708163) SDFをダウンロードする
Smiles	C1=CC(=CC=C1S(=O)(=O)N(CC2=C(C=C(C=C2)C3=NOC=N3)F)C(CCC(F)(F)F)C(=O)N)Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 104 mg/mL ( (199.66 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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