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AZD6482 PI3K 억제제

Name: AZD6482
Brand: Selleck Chemicals
SKU: S1462
Rating: 5 (27 reviews)

제품 번호S1462

AZD6482 (KIN-193)는 PI3Kβ 억제제로, 무세포 분석에서 PI3Kδ, PI3Kα 및 PI3Kγ보다 PI3Kβ에 대해 8배, 87배 및 109배 더 선택적인 IC50 10 nM을 갖습니다. 1상.

화학 구조

분자량: 408.45

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품질 관리

배치: 순도: 99.92%

99.92

관련 타겟	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
기타 PI3K 억제제	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) LY294002 XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549)

세포 배양, 처리 및 작업 농도

세포주	분석 유형	활성 설명
human RXF393 cell	Growth inhibition assay	Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.01154 μM
human SW982 cell	Growth inhibition assay	Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.03584 μM
human MAD-MB-468 cells	Function assay	Inhibition of PI3Kbeta in human MAD-MB-468 cells assessed as inhibition of Ser473 Akt phosphorylation by cellular potency assay, IC50=0.04 μM
human KURAMOCHI cell	Growth inhibition assay	Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=0.1051 μM
human A498 cell	Growth inhibition assay	Inhibition of human A498 cell growth in a cell viability assay, IC50=0.11795 μM
human YT cell	Growth inhibition assay	Inhibition of human YT cell growth in a cell viability assay, IC50=0.12066 μM
human VMRC-RCZ cell	Growth inhibition assay	Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=0.14898 μM
human MDA-MB-415 cell	Growth inhibition assay	Inhibition of human MDA-MB-415 cell growth in a cell viability assay, IC50=0.16732 μM
human J82 cell	Growth inhibition assay	Inhibition of human J82 cell growth in a cell viability assay, IC50=0.47779 μM
human SW1710 cell	Growth inhibition assay	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=0.5292 μM
human T47D cell	Growth inhibition assay	Inhibition of human T47D cell growth in a cell viability assay, IC50=0.5327 μM
human SU-DHL-1 cell	Growth inhibition assay	Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=0.56813 μM
human BT-20 cell	Growth inhibition assay	Inhibition of human BT-20 cell growth in a cell viability assay, IC50=0.59222 μM
human OS-RC-2 cell	Growth inhibition assay	Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=0.62388 μM
human RPMI-6666 cell	Growth inhibition assay	Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=0.64379 μM
human OVCAR-3 cell	Growth inhibition assay	Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=0.67946 μM
human NALM-6 cell	Growth inhibition assay	Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=0.70465 μM
human RS4-11 cell	Growth inhibition assay	Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=0.73806 μM
human SK-MES-1 cell	Growth inhibition assay	Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50=0.78967 μM
human ES7 cell	Growth inhibition assay	Inhibition of human ES7 cell growth in a cell viability assay, IC50=0.81286 μM
human NCI-H2342 cell	Growth inhibition assay	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=0.84294 μM
human SCC-9 cell	Growth inhibition assay	Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=0.8577 μM
human EW-7 cell	Growth inhibition assay	Inhibition of human EW-7 cell growth in a cell viability assay, IC50=0.86356 μM
human HH cell	Growth inhibition assay	Inhibition of human HH cell growth in a cell viability assay, IC50=0.96222 μM
human A427 cell	Growth inhibition assay	Inhibition of human A427 cell growth in a cell viability assay, IC50=0.99505 μM
human Daudi cell	Growth inhibition assay	Inhibition of human Daudi cell growth in a cell viability assay, IC50=1.06888 μM
human P30-OHK cell	Growth inhibition assay	Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=1.07138 μM
human HGC-27 cell	Growth inhibition assay	Inhibition of human HGC-27 cell growth in a cell viability assay， IC50=1.1816 μM
human CAMA-1 cell	Growth inhibition assay	Inhibition of human CAMA-1 cell growth in a cell viability assay, IC50=1.2001 μM
human SK-OV-3 cell	Growth inhibition assay	Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=1.20444 μM
human NCI-H1048 cell	Growth inhibition assay	Inhibition of human NCI-H1048 cell growth in a cell viability assay, IC50=1.22579 μM
human MEL-HO cell	Growth inhibition assay	Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=1.24238 μM
human NKM-1 cell	Growth inhibition assay	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.28636 μM
human NCI-H650 cel	Growth inhibition assay	Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=1.30076 μM
human HAL-01 cell	Growth inhibition assay	Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=1.30175 μM
human 786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.31283 μM
human GI-1 cell	Growth inhibition assay	Inhibition of human GI-1 cell growth in a cell viability assay, IC50=1.31808 μM
human Becker cell	Growth inhibition assay	Inhibition of human Becker cell growth in a cell viability assay, IC50=1.36315 μM
human CCF-STTG1 cell	Growth inhibition assay	Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=1.42525 μM
human MC116 cell	Growth inhibition assay	Inhibition of human MC116 cell growth in a cell viability assay, IC50=1.46122 μM
human MDA-MB-468 cell	Growth inhibition assay	Inhibition of human MDA-MB-468 cell growth in a cell viability assay, IC50=1.53736 μM
human NB12 cell	Growth inhibition assay	Inhibition of human NB12 cell growth in a cell viability assay, IC50=1.54842 μM
human LXF-289 cell	Growth inhibition assay	Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.55104 μM
human MFE-296 cell	Growth inhibition assay	Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=1.56836 μM
human SNU-423 cell	Growth inhibition assay	Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=1.57192 μM
human NCI-H2291 cell	Growth inhibition assay	Inhibition of human NCI-H2291 cell growth in a cell viability assay, IC50=1.5761 μM
human OCUB-M cell	Growth inhibition assay	Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=1.58314 μM
human KU812 cell	Growth inhibition assay	Inhibition of human KU812 cell growth in a cell viability assay, IC50=1.59628 μM
human HuO9 cell	Growth inhibition assay	Inhibition of human HuO9 cell growth in a cell viability assay, IC50=1.6128 μM
human 639-V cell	Growth inhibition assay	Inhibition of human 639-V cell growth in a cell viability assay, IC50=1.63144 μM
human HCC70 cell	Growth inhibition assay	Inhibition of human HCC70 cell growth in a cell viability assay, IC50=1.66146 μM
human SNB75 cell	Growth inhibition assay	Inhibition of human SNB75 cell growth in a cell viability assay, IC50=1.66508 μM
human D-336MG cell	Growth inhibition assay	Inhibition of human D-336MG cell growth in a cell viability assay, IC50=1.6688 μM
human LoVo cell	Growth inhibition assay	Inhibition of human LoVo cell growth in a cell viability assay, IC50=1.73825 μM
human EB2 cell	Growth inhibition assay	Inhibition of human EB2 cell growth in a cell viability assay, IC50=1.75019 μM
human HSC-2 cell	Growth inhibition assay	Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=1.75727 μM
human D-542MG cell	Growth inhibition assay	Inhibition of human D-542MG cell growth in a cell viability assay, IC50=1.85077 μM
human COLO-684 cell	Growth inhibition assay	Inhibition of human COLO-684 cell growth in a cell viability assay, IC50=2.20032 μM
human GDM-1 cell	Growth inhibition assay	Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=2.24206 μM
human SW1088 cell	Growth inhibition assay	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.48143 μM
human SF295 cell	Growth inhibition assay	Inhibition of human SF295 cell growth in a cell viability assay, IC50=2.76955 μM
human NCI-H2030 cell	Growth inhibition assay	Inhibition of human NCI-H2030 cell growth in a cell viability assay, IC50=2.90288 μM
human NCI-H1755 cell	Growth inhibition assay	Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=3.27063 μM
human MDA-MB-361 cell	Growth inhibition assay	Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=3.52709 μM
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	408.45	화학식	C₂₂H₂₄N₄O₄	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1173900-33-8	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	KIN-193			Smiles	CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3C(=O)O)N4CCOCC4

용해도

In vitro
배치:

DMSO : 82 mg/mL (200.75 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 10 mg/mL

Water : Insoluble

DMSO : 82 mg/mL (200.75 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 10 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.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	30.000mg/ml (73.45mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.

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

Targets/IC₅₀/Ki	PI3Kβ (Cell-free assay) 10 nM PI3Kδ (Cell-free assay) 80 nM DNA-PK (Cell-free assay) 420 nM PI3Kα (Cell-free assay) 870 nM
시험관 내(In vitro)	AZD6482는 또한 PI3Kα, γ 및 δ를 억제하며, IC50은 80 nM ~ 1.09 μM으로, 그 (+)-거울상 이성질체(S-형)보다 현저히 낮습니다. 이 화합물은 항혈소판제이며, 세척 혈소판 응집(WPA) 분석에서 혈소판 활성화 접착/응집을 차단하고 혈소판 해리를 촉진하며, IC50 값은 6 nM입니다. 또한, PI3Kβ를 표적으로 하여 이 화학 물질은 정상적인 지혈에 방해 없이 혈전증을 특이적으로 억제합니다. 따라서, 혈전성 질환의 예방을 위한 항혈전제로 사용됩니다.
키나아제 분석	PI3K 효소 억제 분석
키나아제 분석	PI3Kβ, PI3Kα, PI3Kγ 및 PI3Kδ의 억제는 인간 재조합 효소를 사용하는 AlphaScreen 기반 효소 활성 분석에서 평가됩니다. 이 분석은 PI3K 매개 PIP2의 PIP3로의 전환을 측정합니다. 비오틴화된 PIP3, GST 태그가 부착된 플렉스트린 상동성(PH) 도메인 및 두 개의 AlphaScreen 비드는 680 nm에서 레이저 여기 시 신호를 유발하는 복합체를 형성합니다. 효소 반응에서 형성된 PIP3는 PH 도메인에 결합하기 위해 비오틴화된 PIP3와 경쟁하여 효소 생성물이 증가함에 따라 신호를 감소시킵니다. 이 화합물은 DMSO에 용해되어 384웰 플레이트에 첨가됩니다. PBKβ, PBKα, PBKγ 또는 PBKδ는 Tris 버퍼(50 mM Tris pH 7.6, 0.05% CHAPS, 5 mM DTT 및 24 mM MgCl₂)에 첨가되고 PIP2 및 ATP를 포함하는 기질 용액을 첨가하기 전에 이 화학 물질과 20분 동안 사전 배양됩니다. 효소 반응은 EDTA 및 비오틴-PIP3를 포함하는 정지 용액을 첨가한 후 20분 후에 중단되며, 이어서 GST-grpl PH 및 AlphaScreen 비드를 포함하는 검출 용액을 첨가합니다. 플레이트는 분석 전에 최소 5시간 동안 어두운 곳에 보관됩니다. 분석에서 DMSO, ATP 및 PIP2의 최종 농도는 각각 0.8%, 4 μM 및 40 μM입니다. IC50 값은 방정식 y = {a+[(b-a)/(l+(x/IC50)^s)]}에 따라 계산됩니다. 여기서 y = % 억제; a = 0%; b = 100%; s = 농도-반응 곡선의 기울기; x = 이 화합물 농도입니다.
참조	[1] http://www.wipo.int/patentscope/search/en/WO2009093972

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