Name: Sotrastaurin (AEB071)
Brand: Selleck Chemicals
SKU: S2791
Rating: 5 (84 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.97%

99.97

관련 타겟	TGF-beta/Smad ROCK Bcr-Abl
기타 PKC 억제제	Darovasertib (LXS196) PMA chemical (Phorbol 12-myristate 13-acetate) Enzastaurin Go 6983 Bisindolylmaleimide I (GF109203X) Go 6976 Bisindolylmaleimide IX (Ro 31-8220) Mesylate Ruboxistaurin (LY333531) Hydrochloride Rottlerin PKC-theta inhibitor

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
T cell	Function Assay	100 nM	3 h	DMSO	inhibits rRNA synthesis	25691158
HUVECs	Function Assay	500nM	1 h		Reduces DTX-Triggered Endothelial Dysfunction	25634538
A549	Function Assay	0.1 μM	24 h		decreases the relative PKC-α level on cell membrane cotreated AS-IV	25218161
A549	Function Assay	0.1 μM	24 h		reduces the expression levels of MMP-2, MMP-9 and integrin β1	25218161
A549	Growth Inhibition Assay	0.1 μM	24 h		enhances growth inhibition cotreated with AS-IV	25218161
Mel202	Growth Inhibition Assay	0.5 μM	3 h	DMSO	enhances IR-induced reduction in cell viability	24595385
92.1	Growth Inhibition Assay	0.5 μM	3 h	DMSO	enhances IR-induced reduction in cell viability	24595385
OCM3	Growth Inhibition Assay	0.5 μM	3 h	DMSO	enhances IR-induced reduction in cell viability	24595385
Mel202	Growth Inhibition Assay	0.5 μM	3 h	DMSO	increases IR-induced cell cycle arrest	24595385
92.1	Growth Inhibition Assay	0.5 μM	3 h	DMSO	increases IR-induced cell cycle arrest	24595385
OCM3	Growth Inhibition Assay	0.5 μM	3 h	DMSO	increases IR-induced cell cycle arrest	24595385
Jeko-1	Growth Inhibition Assay	0-4 μM		DMSO	inhibits cell growth dose dependently	24362935
Mino	Growth Inhibition Assay	0-4 μM		DMSO	inhibits cell growth dose dependently	24362935
Rec-1	Growth Inhibition Assay	0-4 μM		DMSO	inhibits cell growth dose dependently	24362935
SP49	Growth Inhibition Assay	0-4 μM		DMSO	inhibits cell growth dose dependently	24362935
Jeko-1	Function Assay	2.5 μM	12 h	DMSO	downregulates NF-κB target genes	24362935
Mino	Function Assay	2.5 μM	12 h	DMSO	downregulates NF-κB target genes	24362935
Rec-1	Function Assay	2.5 μM	12 h	DMSO	downregulates NF-κB target genes	24362935
SP49	Function Assay	2.5 μM	12 h	DMSO	downregulates NF-κB target genes	24362935
CD3+ T	Function Assay	0-500 nM	1 h		inhibits NF-κB phosphorylation in a dose dependent manner	23573283
Mel202	Growth Inhibition Assay	0-5 μM	72 h	DMSO	inhibits cell growth dose dependently	22653968
Omm1.3	Growth Inhibition Assay	0-5 μM	72 h	DMSO	inhibits cell growth dose dependently	22653968
92.1	Growth Inhibition Assay	0-5 μM	72 h	DMSO	inhibits cell growth dose dependently	22653968
Mel202	Growth Inhibition Assay	5 μM	24 h	DMSO	induces G1 arrest	22653968
Omm1.3	Growth Inhibition Assay	5 μM	24 h	DMSO	induces G1 arrest	22653968
92.1	Growth Inhibition Assay	5 μM	24 h	DMSO	induces G1 arrest	22653968
Mel202	Apoptosis Assay	5 μM	72 h	DMSO	induces apoptosis slightly	22653968
Omm1.3	Apoptosis Assay	5 μM	72 h	DMSO	induces apoptosis	22653968
92.1	Apoptosis Assay	5 μM	72 h	DMSO	induces apoptosis signifcantly	22653968
Mel202	Function Assay	5 μM	24 h		inhibits expression and phosphorylation of PKC isoforms	22653968
Omm1.3	Function Assay	5 μM	24 h		inhibits expression and phosphorylation of PKC isoforms	22653968
92.1	Function Assay	5 μM	24 h		inhibits expression and phosphorylation of PKC isoforms	22653968
HBL1	Growth Inhibition Assay	0.16-20 μM	5 d		IC50=0.5 μM	21324920
TMD8	Growth Inhibition Assay	0.16-20 μM	5 d		IC50=0.2 μM	21324920
OCI-Ly10	Growth Inhibition Assay	0.16-20 μM	5 d		IC50=1.3 μM	21324920
U2932	Growth Inhibition Assay	0.16-20 μM	5 d		IC50=10 μM	21324920
OCI-Ly3	Growth Inhibition Assay	0.16-20 μM	5 d		IC50＞20 μM	21324920
SuDHL2	Growth Inhibition Assay	0.16-20 μM	5 d		IC50＞20 μM	21324920
SuDHL4	Growth Inhibition Assay	0.16-20 μM	5 d		IC50＞20 μM	21324920
DB	Growth Inhibition Assay	0.16-20 μM	5 d		IC50＞20 μM	21324920
Jurkat IL-2	Growth Inhibition Assay				IC50=6.71 ± 3.76 μM	19940259
PBMC IL-2	Growth Inhibition Assay				IC50=4.84 ± 1.70 μM	19940259
Jurkat	Function assay				Inhibition of TCR/CD28-mediated human T cell activation in Jurkat cells expressing human IL2 promoter by luciferase reporter gene assay, IC50 = 0.054 μM.	19827831
Jurkat T	Function assay		5 hrs		Inhibition of PKCtheta in human Jurkat T cells assessed as reduction in anti-CD3/CD28 antibody-induced T-cell activation by measuring decrease in IL-2 secretion after 5 hrs by luciferase reporter gene assay, IC50 = 0.081 μM.	28131714
B-cells	Function assay				Inhibition of PKCbeta in mouse B cells assessed as reduction in IgM-stimulated cell proliferation, IC50 = 0.234 μM.	28131714
bone marrow cells	Antiproliferative assay		4 days		Antiproliferative activity against CBA mouse bone marrow cells assessed as inhibition of [3H]thymidine incorporation after 4 days, IC50 = 3.7 μM.	19827831
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량	438.48	화학식	C₂₅H₂₂N₆O₂	보관 (수령일로부터)	3년-20°C분말
CAS 번호	425637-18-9	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	CN1CCN(CC1)C2=NC3=CC=CC=C3C(=N2)C4=C(C(=O)NC4=O)C5=CNC6=CC=CC=C65

용해도 (Solubility)

In vitro
배치:

DMSO : 87 mg/mL (198.41 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 40 mg/mL

Water : Insoluble

DMSO : 88 mg/mL (200.69 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 9 mg/mL

Water : Insoluble

DMSO : 87 mg/mL (198.41 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 2 mg/mL

Water : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

특징	Unlike former PKC inhibitors, Sotrastaurin does not enhance apoptosis of murine T-cell blasts in a model of activation-induced cell death.
Targets/IC₅₀/Ki	PKCθ (Cell-free assay) 0.22 nM(Ki) PKCβ1 (Cell-free assay) 0.64 nM(Ki) PKCα (Cell-free assay) 0.95 nM(Ki) PKCη (Cell-free assay) 1.8 nM(Ki) PKCδ (Cell-free assay) 2.1 nM(Ki) PKCε (Cell-free assay) 3.2 nM(Ki)
시험관 내(In vitro)	Treatment with Sotrastaurin (AEB071) at concentrations below 10 μM effectively abrogated markers of early T-cell activation—such as interleukin-2 secretion and CD25 expression—in primary human and mouse T cells at low nanomolar levels. At 200 nM, it inhibits CD3/CD28 antibody- and alloantigen-induced T-cell proliferation without nonspecific antiproliferative effects. Furthermore, this compound (<3 μM) markedly impairs lymphocyte function-associated antigen-1-mediated T-cell adhesion. At concentrations under 20 μM, it selectively impairs the proliferation of CD79 mutant ABC DLBCL cell lines, correlating with reduced NF-κB signaling activity. A concentration of 5 μM induces G1 arrest and/or cell death in CD79 mutant cells.
키나아제 분석	단백질 인산화효소 분석
키나아제 분석	Sotrastaurin (AEB071)은 섬광 근접 분석(scintillation proximity assay) 기술을 사용하여 고전적 및 신규 PKC 이소형에 대해 분석되었습니다. 요약하자면, 이 분석은 20 mM Tris-HCl 완충액(pH 7.4) 및 0.1% 소 혈청 알부민에서 수행되며, 1.5 μM의 펩타이드 기질을 10 μM [³³P]ATP, 10 mM Mg(NO3)₂, 0.2 mM CaCl₂, 25~400 ng/mL의 단백질 농도를 가진 PKC, 그리고 30 mol% 포스파티딜세린, 5 mol% 디아실글리세롤(DAG), 65 mol% 포스파티딜콜린을 함유하여 최종 지질 농도가 0.5 μM인 지질 소낭과 함께 인큐베이션합니다. 인큐베이션은 실온에서 60분 동안 수행됩니다. 반응은 100 mM EDTA, 200 μM ATP, 0.1% Triton X-100 및 Ca²⁺와 Mg²⁺가 없는 PBS 내 0.375 μg/well의 스트렙타비딘 코팅 섬광 근접 분석 비드가 포함된 혼합물 50 μl를 첨가하여 중단됩니다. 포함된 방사능은 MicroBetaTrilux 계수기에서 1분 동안 측정됩니다.
생체 내(In vivo)	In a subcutaneous TMD8 xenograft model in SCID mice, Sotrastaurin (AEB071) (80 mg/kg) results in significant inhibition of in vivo tumor growth. When orally administered at 10 mg/kg and 30 mg/kg b.i.d., this compound shows a dose-dependent immunosuppressive effect leading to pronounced prolongation of heart allograft survival in rats.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/19491325/ [2] https://pubmed.ncbi.nlm.nih.gov/21324920/ [3] https://pubmed.ncbi.nlm.nih.gov/20003043/ [4] https://pubmed.ncbi.nlm.nih.gov/35352024/

적용 분야 (Applications)

방법	바이오마커	이미지	PMID
Western blot	p-Marcks / p-ERK / p-AKT / p-S6 / Marcks / ERK / AKT / S6 PKCα / PKCδ / PKCβ / PKCε / PKCθ Bcl-xl / XIAP / Survivin Cyclin D1 / p27(Kip1) pPKCδ/θ / phosphorylated MARCKS / p53 / MDM2 / PUMA / p21		22653968
Growth inhibition assay	Cell viability		22653968

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT02273219	Completed	Uveal Melanoma	Columbia University	November 19 2014	Phase 1
NCT01801358	Terminated	Uveal Melanoma	Array Biopharma now a wholly owned subsidiary of Pfizer\|Array BioPharma	August 2013	Phase 1\|Phase 2
NCT01430416	Completed	Uveal Melanoma	Novartis Pharmaceuticals\|Novartis	December 20 2011	Phase 1
NCT01402440	Terminated	Diffuse Large B-Cell Lymphoma	Novartis Pharmaceuticals\|Novartis	November 2011	Phase 1

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
Could you give me the information about how to prepare it for oral administration in mice?

답변:
It can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as a clear solution which can be used for injection, and in 2% DMSO/corn oil at 10 mg/ml as a suspension for oral administration.

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):

Sotrastaurin (AEB071) PKC inhibitor

화학 구조

분자량: 438.48

품질 관리 (Quality Control)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

자주 묻는 질문 (Frequently Asked Questions)

Sotrastaurin (AEB071) PKC inhibitor

화학 구조

분자량: 438.48

품질 관리 (Quality Control)

세포 배양, 처리 및 작업 농도 (Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

자주 묻는 질문 (Frequently Asked Questions)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)