Home JAK/STAT JAK inhibitor WP1066

연구용

WP1066 JAK2/STAT3 Inhibitor

제품 번호S2796

WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1.
WP1066 JAK inhibitor Chemical Structure

화학 구조

분자량: 356.22

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품질 관리 (Quality Control)

배치: 순도: 99.97%
99.97

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
human MM1 cells Function assay 24-72 h Antitumor activity against human MM1 cells after 24 to 72 hrs by MTT assay, ic50=1.2 μM
human U266 cells Function assay 24-72 h Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay, IC50=1.5 μM
human OCI-My4 cells Function assay 24-72 h Antitumor activity against human OCI-My4 cells after 24 to 72 hrs by MTT assay, IC50=1.8 μM
human 30M cells Cytotoxic assay 8 days Cytotoxicity against human 30M cells assessed as cell viability after 8 days by Alamar Blue assay, IC50=1.8 μM
human 73M cells Cytotoxic assay 8 days Cytotoxicity against human 73M cells assessed as cell viability after 8 days by Alamar Blue assay, IC50=2.1 μM
human U373MG cells Function assay 24-72 h Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay, IC50=3.7 μM
human U87MG cells Function assay 24-72 h Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay, IC50=5.6 μM
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 356.22 화학식

C17H14BrN3O

 보관 (수령일로부터)
CAS 번호 857064-38-1 SDF 다운로드 원액 보관

동의어 N/A Smiles CC(C1=CC=CC=C1)NC(=O)C(=CC2=NC(=CC=C2)Br)C#N

용해도 (Solubility)

In vitro
배치:

DMSO : 71 mg/mL (199.31 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
Similar to its parent compound AG490, WP1066 inhibits the phosphorylation of JAK2, but unlike AG490, WP1066 also degraded JAK2 protein.
Targets/IC50/Ki
JAK2
(HEL cells)
2.3 μM
STAT3
(HEL cells)
2.43 μM
시험관 내(In vitro)
WP1066 markedly inhibits the growth of HEL cells carrying the JAK2 V617F mutant isoform in a dose-dependent manner with IC20, IC50 and IC80 of 0.8, 2.3 and 3.8 μM. This compound at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μM inhibits the phosphorylation of JAK2, STAT3, STAT5, and ERK1/2 without affecting the phosphorylation of JAK1 and JAK3 in erythroid leukemia HEL cells that express the JAK2 V617F isoform. It at concentrations ranging from 0.5 to 3.0 μM inhibits the proliferation of AML colony-forming cells obtained from patients and that of the AML cell lines OCIM2 and K562 in a dose-dependent manner. This chemical at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μM dose-dependently decreases JAK2 and pJAK2 protein levels as well as downstream phosphorylation levels of STAT3, STAT5, and AKT in OCIM2 and K562 cells. It at concentrations of 2 μM inhibits OCIM2 cell multiplication by inducing accumulation of cells at the G0-G1 phase of the cell cycle. This compound at concentrations of 1, 2, or 3 μM induces apoptosis in both OCIM2 and K562 cells in a dose-dependent fashion by activating procaspase-3 and cleaving PARP. It at concentrations of 5 μM prevents the phosphorylation of STAT3, and at concentrations of 2.5μM it significantly inhibits cell survival and proliferation in Caki-1 and 786-O renal cancer cells. This chemical at concentrations of 5 μM suppresses HIF1α and HIF2α expression and VEGF production in Caki-1 and 786-O renal cancer cells.
생체 내(In vivo)
WP1066 orally administrated at dose of 40 mg/kg once daily for 19 days significantly inhibits the tumours growth in Caki-1 xenograft mice, with decreased immunostaining of phosphorylated STAT3 and reduced length of CD34-positive vessels.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/20461084/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot p-STAT3 / STAT3 / p-ERK / ERK
S2796-WB1
20461084
Cell viability Cell viability
S2796-viability1
28496056
Immunofluorescence N-cadherin / E-cadherin / Vimentin / β-catenin
S2796-IF1
26690371

임상시험 정보 (Clinical Trial Information)

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

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT04334863 Completed
Brain Tumor|Medulloblastoma|Brain Metastases
Emory University|CURE Childhood Cancer Inc.|Peach Bowl LegACy Fund
 May 4 2020 Phase 1