Name: AT9283
Brand: Selleck Chemicals
SKU: S1134
Rating: 5 (36 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.82%

99.82

관련 타겟	EGFR STAT Pim
기타 JAK 억제제	BMS-986165 (Deucravacitinib) AZD1480 WP1066 Momelotinib (CYT387) Filgotinib (GLPG0634) Gandotinib (LY2784544) Pacritinib (SB1518) NVP-BSK805 2HCl TG101209 Cerdulatinib (PRT062070) hydrochloride

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

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
HCT116	Cytotoxicity assay		10 to 14 days	Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay, IC50=0.012μM	19143567
HCT116	Function assay	10 mg/kg		Cmax in BALB/c mouse bearing human HCT116 cells at 10 mg/kg, po, Cmax=0.45μM	19143567
HCT116	Function assay	5 mg/kg		Cmax in BALB/c mouse bearing human HCT116 cells at 5 mg/kg, iv, Cmax=4.9μM	19143567
HCT116	Function assay	20 mg/kg		Cmax in BALB/c mouse bearing human HCT116 cells at 20 mg/kg, ip, Cmax=8.4μM	19143567
HT-29	Antitumor assay		72 hrs	Antitumor activity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.383μM	23664099
A549	Antitumor assay		72 hrs	Antitumor activity against human A549 cells after 72 hrs by MTT assay, IC50=0.512μM	23664099
LoVo	Antitumor assay		72 hrs	Antitumor activity against human LoVo cells after 72 hrs by MTT assay, IC50=0.553μM	23664099
K562	Antitumor assay		72 hrs	Antitumor activity against human K562 cells after 72 hrs by MTT assay, IC50=1.6μM	23664099
U937	Antitumor assay		72 hrs	Antitumor activity against human U937 cells after 72 hrs by MTT assay, IC50=6.7μM	23664099
BL21 (DE3)	Function assay		30 mins	Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method, IC50=0.685μM	28351607
Sf9	Function assay			Binding affinity to N-terminal TEV-cleavable hexa-histidine tagged human JAK2 JH1 domain (840 to 1132 residues) expressed in baculovirus-infected Sf9 cells by ITC assay, Kd=0.011μM	28626521
Sf9	Function assay			Binding affinity to C-terminal thrombin-cleavable hexa-histidine tagged human JAK2 JH2 pseudokinase domain (536 to 812 residues) W659A/W777A/F794H mutant expressed in baculovirus-infected Sf9 cells by ITC assay, Kd=1.323μM	28626521
Sf9	Function assay	10 uM	60 mins	Displacement of BODIPY-ATP from C-terminal thrombin-cleavable hexa-histidine tagged human JAK2 JH2 pseudokinase domain (536 to 812 residues) W659A/W777A/F794H mutant expressed in baculovirus-infected Sf9 cells at 10 uM after 60 mins by high-throughput flu	28626521
HCT116	Function assay			Inhibition of Aurora B kinase in human HCT116 cells assessed as reduction in polyploid phenotype, IC50=0.03μM	28918096
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
클릭하여 더 많은 세포주 실험 데이터 보기

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

분자량	381.43	화학식	C₁₉H₂₃N₇O₂	보관 (수령일로부터)	3년-20°C분말
CAS 번호	896466-04-9	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	C1CC1NC(=O)NC2=C(NN=C2)C3=NC4=C(N3)C=C(C=C4)CN5CCOCC5

용해도 (Solubility)

In vitro
배치:

DMSO : 76 mg/mL (199.25 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 25 mg/mL

Water : Insoluble

DMSO : 76 mg/mL (199.25 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 76 mg/mL

Water : Insoluble

DMSO : 76 mg/mL (199.25 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 38 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)

Targets/IC₅₀/Ki	JAK3 (Cell-free assay) 1.1 nM JAK2 (Cell-free assay) 1.2 nM Aurora A (Cell-free assay) ~3.0 nM Aurora B (Cell-free assay) ~3.0 nM Abl1 (T315I) (Cell-free assay) 4 nM GSK-3β (Cell-free assay) 1 nM-10 nM FGFR2 (Cell-free assay) 1-10 nM VEGFR3/FLT4 (Cell-free assay) 1 nM-10 nM Mer (Cell-free assay) 1 nM-10 nM RET (Cell-free assay) 1 nM-10 nM RSK2 (Cell-free assay) 1 nM-10 nM RSK3 (Cell-free assay) 1 nM-10 nM TYK2 (Cell-free assay) 1 nM-10 nM YES (Cell-free assay) 1 nM-10 nM Abl (Q252H) (Cell-free assay) 10 nM-30 nM DRAK1 (Cell-free assay) 10 nM-30 nM FGFR1 (Cell-free assay) 10 nM-30 nM FGFR1 (V561M) (Cell-free assay) 10 nM-30 nM FGFR2 (N549H) (Cell-free assay) 10 nM-30 nM FGFR3 (Cell-free assay) 10 nM-30 nM VEGFR1/FLT1 (Cell-free assay) 10 nM-30 nM FLT3 (Cell-free assay) 10 nM-30 nM PDGFRα (D842V) (Cell-free assay) 10 nM-30 nM PDK-1 (Cell-free assay) 10 nM-30 nM PKCμ (Cell-free assay) 10 nM-30 nM RSK4 (Cell-free assay) 10 nM-30 nM Src (T341M) (Cell-free assay) 10 nM-30 nM VEGFR2 (Cell-free assay) 10 nM-30 nM
시험관 내(In vitro)	AT9283 leads to a clear polyploid phenotype by inhibiting the activity of Aurora B kinase in HCT116 cells with IC50 of 30 nM. Furthermore, this compound also produces the potent inhibition on HCT116 colony formation.
키나아제 분석	Aurora A 및 Aurora B Kinase 분석
키나아제 분석	Aurora A 및 B에 대한 분석은 DELFIA 형식으로 수행됩니다. Aurora A 효소를 10 mM MOPS(pH 7), 0.1 mg/mL BSA, 0.001% Brij-35, 0.5% 글리세롤, 0.2 mM EDTA, 10 mM MgCl₂, 0.01% β-머캅토에탄올, 15 μM ATP 및 2.5% DMSO 내에서 AT9283 및 3 μM cross-tide 기질(biotin-CGPKGPGRRGRRRTSSFAEG)과 함께 인큐베이션합니다. Aurora B 효소를 25 mM Tris(pH 8.5), 5 mM MgCl₂, 0.1 mg/mL BSA, 0.025% Tween-20, 1 mM DTT, 15 μM ATP 및 2.5% DMSO 내에서 본 화합물 및 3 μM의 상기 기질과 함께 인큐베이션합니다. 반응은 EDTA로 퀀칭하기 전까지 Aurora A의 경우 60분, Aurora B의 경우 45~90분 동안 진행됩니다. 그 후 반응 혼합물을 뉴트라비딘(neutravidin) 코팅 플레이트로 옮기고, 인산화된 펩타이드를 인산화 특이적 항체와 유로퓸 표지 이차 항체를 사용하여 시간 분해 형광(들뜸 337 nm, 방출 620 nm) 방식으로 정량합니다. 대조 화합물에 대한 IC50 값은 92 nM(Aurora A 분석) 및 17 nM(Aurora B)입니다.
생체 내(In vivo)	In HCT116 human colon carcinoma xenograft bearing mice, AT9283 treatment (15 mg/kg and 20 mg/kg) for 16 days results in a significant tumor growth inhibition of 67% and 76%, respectively. In addition, this compound also exhibits a significantly longer half-life in tumors(2.5 hours) compared with plasma (0.5 hour) and modest oral bioavailability in mice (Fp.o. = 24%).
참조	[1] https://pubmed.ncbi.nlm.nih.gov/19143567/ [2] https://pubmed.ncbi.nlm.nih.gov/21796626/ [3] https://pubmed.ncbi.nlm.nih.gov/21430070/

적용 분야 (Applications)

방법	바이오마커	이미지	PMID
Growth inhibition assay	Cell viability		21430070

임상시험 정보 (Clinical Trial Information)

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT01145989	Completed	Multiple Myeloma	NCIC Clinical Trials Group\|Astex Pharmaceuticals Inc.\|Canadian Cancer Trials Group	February 15 2011	Phase 2
NCT00443976	Completed	Non-Hodgkins Lymphoma\|Unspecified Adult Solid Tumor Protocol Specific	NCIC Clinical Trials Group\|Astex Pharmaceuticals Inc.\|Canadian Cancer Trials Group	January 30 2007	Phase 1

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):

AT9283 Multikinase Inhibitor

화학 구조

분자량: 381.43

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)

AT9283 Multikinase Inhibitor

화학 구조

분자량: 381.43

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)

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