Home MAPK ERK inhibitor SCH772984

연구용

SCH772984 ERK1/2 inhibitor

제품 번호: S7101

SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells.
SCH772984 ERK inhibitor Chemical Structure

화학 구조

분자량: 587.67

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품질 관리 (Quality Control)

배치: 순도: 99.99%
99.99

함께 자주 사용되는 제품 SCH772984

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Phenformin HCl

Phenformin enhances its antiproliferative activity in Mewo, M308, and SK-Mel-113 cells.

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
2P-ERK2 Growth Inhibition Assay IC50=0.24 nM 25350931
A375 Function assay 2 hrs Inhibition of ERK2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-ERK2 level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50 = 0.004 μM. 25977981
A375 Function assay Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated ERK2 levels, IC50 = 0.004 μM. 28376306
COLO205 Antiproliferative assay 4 days Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days, IC50 = 0.016 μM. 30034615
A375 Function assay 2 hrs Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50 = 0.02 μM. 25977981
A375 Function assay 2 hrs Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50 = 0.02 μM. 25977981
A375 Function assay Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated RSK levels, IC50 = 0.02 μM. 28376306
HT-29 Antiproliferative assay 4 days Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days, IC50 = 0.059 μM. 30034615
HT-29 Antiproliferative assay Antiproliferative activity against human HT-29 cells harboring BRAF/KRAS mutant, IC50 = 0.059 μM. 29748051
A375 Antiproliferative assay 72 hrs Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50 = 0.07 μM. 25977981
HT-29 Apoptosis assay Induction of apoptosis in human HT-29 cells harboring BRAF/KRAS mutant by caspase activation assay, IC50 = 0.096 μM. 29748051
클릭하여 더 많은 세포주 실험 데이터 보기

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

분자량 587.67 화학식

C33H33N9O2

 보관 (수령일로부터)
CAS 번호 942183-80-4 SDF 다운로드 원액 보관

동의어 N/A Smiles C1CN(CC1C(=O)NC2=CC3=C(C=C2)NN=C3C4=CC=NC=C4)CC(=O)N5CCN(CC5)C6=CC=C(C=C6)C7=NC=CC=N7

용해도 (Solubility)

In vitro
배치:

DMSO : 14 mg/mL (23.82 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

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

mg/kg g μL

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
Does not directly inhibit MEK1, MEK2, BRAF, or CRAF enzyme activity.
Targets/IC50/Ki
ERK2
(Cell-free assay)
1 nM
ERK1
(Cell-free assay)
4 nM
시험관 내(In vitro)
SCH772984 is a novel, selective and ATP competitive inhibitor of ERK1/2. This compound inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner. It also inhibits phosphorylation of residues in the activation loop of ERK itself. This inhibitor demonstrates EC50 values <500 nM in approximately 88% and 49% of BRAF-mutant or RAS-mutant tumor lines, respectively. Importantly, it effectively inhibited MAPK signaling and cell proliferation in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors.
키나아제 분석
ERK2 IMAP enzymatic assay
SCH772984 is tested in 8 point dilution curves in duplicate against purified ERK2 or ERK1. The enzyme is added to the reaction plate. and incubated with this compound before adding a solution of substrate peptide and ATP. 14μl of diluted enzyme (0.3ng active ERK2 per reaction) is added to each well of a 384-well plate. The plates are gently shaken to mix the reagents and incubated for 45 minutes at room temperature. The reaction is stopped with 60μl of IMAP Binding Solution (1:2200 dilutions of IMAP beads in 1X Binding Buffer). The plates are incubated at room temperature for an additional 0.5 hours to allow complete binding of phosphopeptides to the IMAP beads. Plates are read on the LJL Analyst.
생체 내(In vivo)
SCH772984 induces tumor regressions in xenograft models at tolerated doses. This compound effectively inhibites MAPK signaling and cell proliferation in BRAF or MEK inhibitor resistant models.
참조

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot cyclin B1 / cyclin D1 / p21 pRSK / pERK / pAKT / pMEK DUSP1 / DUSP4 / DUSP6 pCRAF(S338, S289, S296, S301) Aurora B / ETS1 / ETS2
S7101-WB1
26725216
Growth inhibition assay Cell viability
S7101-viability1
30118499
Immunofluorescence TOMM20 pERK1/2
S7101-IF1
30833752

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
I would like to inhibit Erk1/2 by treating the mice with it. By what kind of administration way and at what concentration could this compound be used?

답변:
It can be administered by I.P. The dosages can be used as: 12.5 mg/kg, 25 mg/kg, 50 mg/kg. For more detailed information please find the paper below: http://cancerdiscovery.aacrjournals.org/content/3/7/742.full