Afuresertib (GSK2110183)

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with K_i of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

CAS No. 1047644-62-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 71500	国内在庫あり
100mg	JPY 149500	国内在庫あり
1g	JPY 448500	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

文献中Selleckの製品使用例（31）

製品安全説明書

現在のバッチを見る：純度： 99.61%

99.61

Afuresertib (GSK2110183)関連製品

関連ターゲット	Akt1 Akt2 Akt3	もっと見る
関連製品	MK-2206 2HCl Perifosine SC79 Capivasertib (AZD5363) GSK690693 Ipatasertib (GDC-0068) Triciribine (API-2) CCT128930 A-674563 HCl AT7867 Oridonin Akti-1/2 PHT-427 TIC10 (ONC201) Miransertib (ARQ 092) HCl Miltefosine AT13148 Uprosertib (GSK2141795) Miransertib (ARQ-092) SC66 Deguelin ML-9 HCl	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	もっと見る

シグナル伝達経路

Aktシグナル伝達経路

Akt阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
Sf9	Function assay	40 mins	Inhibition of full length human AKT1 expressed in Sf9 cells assessed as reduction in substrate phosphorylation using biotin-ahx-ARKRERAYSFGHHA-amide substrate and [gamma-33P]ATP incubated for 40 mins by top count microplate scintillation counting method, IC50 = 0.001 μM.	ChEMBL
Sf9	Function assay	40 mins	Inhibition of full length human AKT3 expressed in Sf9 cells assessed as reduction in substrate phosphorylation using biotin-ahx-ARKRERAYSFGHHA-amide substrate and [gamma-33P]ATP incubated for 40 mins by top count microplate scintillation counting method, IC50 = 0.001585 μM.	ChEMBL
COLO205	Growth inhibition assay	72 hrs	Growth inhibition of human COLO205 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs , IC50 = 0.009 μM.	ChEMBL
Sf9	Function assay	40 mins	Inhibition of full length human AKT2 expressed in Sf9 cells assessed as reduction in substrate phosphorylation using biotin-ahx-ARKRERAYSFGHHA-amide substrate and [gamma-33P]ATP incubated for 40 mins by top count microplate scintillation counting method, IC50 = 0.01 μM.	ChEMBL
MV522	Growth inhibition assay	72 hrs	Growth inhibition of human MV522 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.012 μM.	ChEMBL
HT-29	Growth inhibition assay	72 hrs	Growth inhibition of human HT-29 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.015 μM.	ChEMBL
NCI-H727	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H727 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.019 μM.	ChEMBL
SW1417	Growth inhibition assay	72 hrs	Growth inhibition of human SW1417 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.03 μM.	ChEMBL
Calu6	Growth inhibition assay	72 hrs	Growth inhibition of human Calu6 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.031 μM.	ChEMBL
LS1034	Growth inhibition assay	72 hrs	Growth inhibition of human LS1034 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.04 μM.	ChEMBL
SW1463	Growth inhibition assay	72 hrs	Growth inhibition of human SW1463 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.041 μM.	ChEMBL
RKO	Growth inhibition assay	72 hrs	Growth inhibition of human RKO cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.054 μM.	ChEMBL
NCI-H508	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H508 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.08 μM.	ChEMBL
NCI-H1155	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H1155 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hr, IC50 = 0.101 μM.	ChEMBL
A427	Growth inhibition assay	72 hrs	Growth inhibition of human A427 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.103 μM.	ChEMBL
KM12	Growth inhibition assay	72 hrs	Growth inhibition of human KM12 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.104 μM.	ChEMBL
HCT8	Growth inhibition assay	72 hrs	Growth inhibition of human HCT8 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.143 μM.	ChEMBL
MDA-MB-175-VII	Growth inhibition assay	72 hrs	Growth inhibition of human MDA-MB-175-VII cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.155 μM.	ChEMBL
A549	Growth inhibition assay	72 hrs	Growth inhibition of human A549 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.164 μM.	ChEMBL
NCI-H23	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H23 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs , IC50 = 0.199 μM.	ChEMBL
SW837	Growth inhibition assay	72 hrs	Growth inhibition of human SW837 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.248 μM.	ChEMBL
SW480	Growth inhibition assay	72 hrs	Growth inhibition of human SW480 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.259 μM.	ChEMBL
NCI-H1355	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H1355 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hr, IC50 = 0.268 μM.	ChEMBL
EFM19	Growth inhibition assay	72 hrs	Growth inhibition of human EFM19 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.3 μM.	ChEMBL
T84	Growth inhibition assay	72 hrs	Growth inhibition of human T84 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.304 μM.	ChEMBL
COR-L23	Growth inhibition assay	72 hrs	Growth inhibition of human COR-L23 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs , IC50 = 0.368 μM.	ChEMBL
NCI-H1792	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H1792 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hr, IC50 = 0.374 μM.	ChEMBL
SW1573	Growth inhibition assay	72 hrs	Growth inhibition of human SW1573 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.382 μM.	ChEMBL
Calu3	Growth inhibition assay	72 hrs	Growth inhibition of human Calu3 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.392 μM.	ChEMBL
HCC827	Growth inhibition assay	72 hrs	Growth inhibition of human HCC827 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.401 μM.	ChEMBL
EFM19	Growth inhibition assay	72 hrs	Growth inhibition of human EFM19 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 0.43 μM.	ChEMBL
HOP62	Growth inhibition assay	72 hrs	Growth inhibition of human HOP62 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.498 μM.	ChEMBL
NCI-H508	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H508 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 0.522 μM.	ChEMBL
SW900	Growth inhibition assay	72 hrs	Growth inhibition of human SW900 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.719 μM.	ChEMBL
MDA-MB-175-VII	Growth inhibition assay	72 hrs	Growth inhibition of human MDA-MB-175-VII cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 0.794 μM.	ChEMBL
NCI-H1155	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H1155 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 0.865 μM.	ChEMBL
DLD1	Growth inhibition assay	72 hrs	Growth inhibition of human DLD1 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.932 μM.	ChEMBL
HT-29	Growth inhibition assay	72 hrs	Growth inhibition of human HT-29 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 1.383 μM.	ChEMBL
HCT8	Growth inhibition assay	72 hrs	Growth inhibition of human HCT8 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 1.541 μM.	ChEMBL
RKO	Growth inhibition assay	72 hrs	Growth inhibition of human RKO cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 1.806 μM.	ChEMBL
Calu6	Growth inhibition assay	72 hrs	Growth inhibition of human Calu6 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 2.154 μM.	ChEMBL
KM12	Growth inhibition assay	72 hrs	Growth inhibition of human KM12 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 2.247 μM.	ChEMBL
COLO205	Growth inhibition assay	72 hrs	Growth inhibition of human COLO205 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 2.567 μM.	ChEMBL
MV522	Growth inhibition assay	72 hrs	Growth inhibition of human MV522 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 3.044 μM.	ChEMBL
LS1034	Growth inhibition assay	72 hrs	Growth inhibition of human LS1034 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 4.339 μM.	ChEMBL
NCI-H727	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H727 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 4.799 μM.	ChEMBL
COR-L23	Growth inhibition assay	72 hrs	Growth inhibition of human COR-L23 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 5.373 μM.	ChEMBL
A549	Growth inhibition assay	72 hrs	Growth inhibition of human A549 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 5.993 μM.	ChEMBL
NCI-H1355	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H1355 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 6.685 μM.	ChEMBL
NCI-H23	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H23 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 7.124 μM.	ChEMBL
NCI-H1792	Growth inhibition assay	72 hrs	Growth inhibition of human NCI-H1792 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 7.307 μM.	ChEMBL
SW1463	Growth inhibition assay	72 hrs	Growth inhibition of human SW1463 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 9.725 μM.	ChEMBL
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生物活性

製品説明

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with K_i of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

Targets

Akt1 ^[1] (Cell-free assay)	Akt2 ^[1] (Cell-free assay)	Akt3 ^[1] (Cell-free assay)
0.08 nM(Ki)	2 nM(Ki)	2.6 nM(Ki)

In Vitro
In vitro	Afuresertib inhibits the kinase activity of the E17K AKT1 mutant protein with EC50 of 0.2 nM. Afuresertib shows a concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3b, PRAS40, FOXO and Caspase 9. Overall 65% of the hematological cell lines are sensitive to afuresertib (EC50 < 1 μM). Among tested solid tumor cell lines, 21% have EC50 < 1 μM in response to afuresertib.^[1]
Kinase Assay	Potency (Ki*) of afuresertib
Kinase Assay	The true potency (Ki*) of the inhibitor is initially determined at low enzyme concentrations (0.1 nM AKT1, 0.7 nM AKT2, and 0.2 nM AKT3) using a filter binding assay and then confirmed with progress curve analysis. In the filter binding assay, a pre-mix of enzyme plus inhibitor is incubated for 1 h and then added to a GSKα peptide (Ac-KKGGRARTSS-FAEPG-amide) and [γ³³P] ATP. Reactions are terminated after 2 h and the radio labeled AKT peptide product is captured in a phospho-cellulose filter plate. Progress curve analysis utilizes continuous real-time fluorescence detection of product formation using the Sox-AKT-tide substrate (Ac-ARKRERAYSF-d-Pro-Sox-Gly-NH2).
細胞実験	細胞株	Hematological cell lines and solid tumor cell lines
	濃度	30 μM
	反応時間	72 h
	実験の流れ	A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth inhibition by the compounds at 0-30 μM. Cell growth is determined relative to untreated (DMSO) controls. EC50’s are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	p-GSK3 / GSK3 / p-PRAS40 / PRAS40 / p-FOXO / p-Casp9 / p-AKT / AKT / p-MEK / p-ERK / Erk ATG3 / ATG12 / LC3B		24978597

In Vivo
In Vivo	Mice bearing BT474 breast tumor xenografts are dosed with afuresertib (p.o.) at 10, 30 or 100 mg/kg daily which results in 8, 37 and 61% TGI, respectively. Mice bearing SKOV3 ovarian tumor xenografts are treated with 10, 30 and 100 mg/kg afuresertib which results in 23, 37 and 97% TGI, respectively.^[1]
動物実験	動物モデル	Female athymic nude and SCID mice bearing SKOV3 or BT474 tumors
	投与量	100 mg/kg
	投与経路	p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05489744	Completed	Healthy Volunteer	Laekna Limited	August 6 2022	Phase 1
NCT04374630	Active not recruiting	Platinum-resistant Ovarian Cancer	Laekna Limited	June 9 2020	Phase 2
NCT04060394	Active not recruiting	Metastatic Castration-resistant Prostate Cancer	Laekna Limited	September 13 2019	Phase 1\|Phase 2
NCT02235740	Terminated	Cancer	Novartis\|Amgen	November 2014	Phase 1

参考
[1] Dumble M, et al. PLoS One, 2014, 9(6):e100880.

参考

[1] Dumble M, et al. PLoS One, 2014, 9(6):e100880.

化学情報

分子量	427.32	化学式	C₁₈H₁₇Cl₂FN₄OS
CAS No.	1047644-62-1	SDF	Download Afuresertib (GSK2110183) SDFをダウンロードする
Smiles	CN1C(=C(C=N1)Cl)C2=C(SC(=C2)C(=O)NC(CC3=CC(=CC=C3)F)CN)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 : 85 mg/mL ( (198.91 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。)

Ethanol : 85 mg/mL

Water : 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。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):