Home MAPK p38 MAPK 억제제 VX-702

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VX-702 p38 MAPK 억제제

제품 번호S6005

VX-702는 p38α MAPK의 고도로 선택적인 억제제로, p38β에 비해 p38α에 대한 효능이 14배 더 높습니다.
VX-702 p38 MAPK 억제제 Chemical Structure

화학 구조

분자량: 404.3

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품질 관리

배치: 순도: 99.94%
99.94

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.01543 μM
human NCI-H720 cell Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=0.01682 μM
JVM-2 cell Growth inhibition assay Inhibition of human JVM-2 cell growth in a cell viability assay, IC50=0.083 μM
human NCI-H69 cell Growth inhibition assay Inhibition of human NCI-H69 cell growth in a cell viability assay, IC50=0.09941 μM
human BV-173 cell Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=0.11386 μM
human KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=0.12488 μM
human DU-145 cell Growth inhibition assay Inhibition of human DU-145 cell growth in a cell viability assay, IC50=0.14554 μM
KARPAS-45 cell Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=0.14826 μM
human AGS cell Growth inhibition assay Inhibition of human AGS cell growth in a cell viability assay, IC50=0.15251 μM
human MOLT-13 cell Growth inhibition assay Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=0.15981 μM
human NCI-H209 cell Growth inhibition assay Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=0.1758 μM
human CTV-1 cell Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=0.18389 μM
LU-139 cell Growth inhibition assay Inhibition of human LU-139 cell growth in a cell viability assay, IC50=0.19435 μM
ML-2 cell Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50=0.22661 μM
human K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50=0.22917 μM
human SBC-1 cell Growth inhibition assay Inhibition of human SBC-1 cell growth in a cell viability assay, IC50=0.2362 μM
human COR-L88 cell Growth inhibition assay Inhibition of human COR-L88 cell growth in a cell viability assay, IC50=0.3348 μM
human KY821 cell Growth inhibition assay Inhibition of human KY821 cell growth in a cell viability assay, IC50=0.39603 μM
human HCC2218 cell Growth inhibition assay Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=0.49728 μM
human ECC10 cell Growth inhibition assay Inhibition of human ECC10 cell growth in a cell viability assay, IC50=0.65389 μM
human EW-3 cell Growth inhibition assay Inhibition of human EW-3 cell growth in a cell viability assay, IC50=0.66611 μM
human EW-18 cell Growth inhibition assay Inhibition of human EW-18 cell growth in a cell viability assay, IC50=0.74679 μM
human UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=1.20326 μM
human G-361 cell Growth inhibition assay Inhibition of human G-361 cell growth in a cell viability assay, IC50=1.49519 μM
human HMV-II cell Growth inhibition assay Inhibition of human HMV-II cell growth in a cell viability assay, IC50=1.77184 μM
human DEL cell Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay, IC50=2.20704 μM
human IGROV-1 cell Growth inhibition assay Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=2.43188 μM
human SK-OV-3 cell Growth inhibition assay Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=2.61697 μM
human LAMA-84 cell Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=2.71284 μM
human NCI-H510A cell Growth inhibition assay Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50=2.92526 μM
human CP66-MEL cell Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=2.93559 μM
human HAL-01 cell Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=3.27918 μM
human RS4-11 cell  Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=3.70573 μM
human RPMI-8226 cell Growth inhibition assay Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50=3.82376 μM
human NCI-H82 cell Growth inhibition assay Inhibition of human NCI-H82 cell growth in a cell viability assay, IC50=3.89305 μM
human NY cells Growth inhibition assay Inhibition of human NY cell growth in a cell viability assay, IC50=4.27637 μM
human MDA-MB-361 cell Growth inhibition assay Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=4.43158 μM
human MOLT-4 cell Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=4.99193 μM
human DU-4475 cell Growth inhibition assay Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=5.05565 μM
human ESS-1 cell Growth inhibition assay Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=5.29179 μM
human NCI-H1299 cell Growth inhibition assay Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=5.53033 μM
human COLO-684 cell Growth inhibition assay Inhibition of human COLO-684 cell growth in a cell viability assay, IC50=5.58165 μM
human MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=5.71199 μM
human D-542MG cell Growth inhibition assay Inhibition of human D-542MG cell growth in a cell viability assay, IC50=6.39272 μM
human A4-Fuk cell Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=6.43662 μM
human HL-60 cell Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50=7.52212 μM
human NCI-H526 cell Growth inhibition assay Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50=7.59801 μM
human L-363 cell Growth inhibition assay Inhibition of human L-363 cell growth in a cell viability assay, IC50=7.79252 μM
human A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=7.80384 μM
human MS-1 Growth inhibition assay Inhibition of human MS-1 cell growth in a cell viability assay, IC50=7.83465 μM
human JAR cell Growth inhibition assay Inhibition of human JAR cell growth in a cell viability assay, IC50=7.84923 μM
human TI-73 cell Growth inhibition assay Inhibition of human TI-73 cell growth in a cell viability assay, IC50=8.0622 μM
human CTB-1 cell Growth inhibition assay Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=8.17825 μM
human SK-NEP-1 cell Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=11.3038 μM
human HT-29 cell Growth inhibition assay Inhibition of human HT-29 cell growth in a cell viability assay, IC50=13.9111 μM
human NCI-H1092 cell Growth inhibition assay Inhibition of human NCI-H1092 cell growth in a cell viability assay, IC50=14.318 μM
human KMOE-2 cell Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50=14.6178 μM
human EM-2 cell Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=15.2841 μM
human RT-112 cell Growth inhibition assay Inhibition of human RT-112 cell growth in a cell viability assay, IC50=15.3984 μM
human DB cell Growth inhibition assay Inhibition of human DB cell growth in a cell viability assay, IC50=15.8513 μM
human NCI-H1770 cell Growth inhibition assay Inhibition of human NCI-H1770 cell growth in a cell viability assay
human CAL-54 cell Growth inhibition assay Inhibition of human CAL-54 cell growth in a cell viability assay, IC50=16.73 μM
human NB14 cell Growth inhibition assay Inhibition of human NB14 cell growth in a cell viability assay, IC50=17.6395 μM
human RPMI-7951 cell Growth inhibition assay Inhibition of human RPMI-7951 cell growth in a cell viability assay, IC50=19.1783 μM
human T47D cell Growth inhibition assay Inhibition of human T47D cell growth in a cell viability assay, IC50=21.2243 μM
human A549 cell Growth inhibition assay Inhibition of human A549 cell growth in a cell viability assay, IC50=21.2811 μM
human A2780 cell Growth inhibition assay Inhibition of human A2780 cell growth in a cell viability assay, IC50=21.8225 μM
human SK-MEL-24 cell Growth inhibition assay Inhibition of human SK-MEL-24 cell growth in a cell viability assay, IC50=33.0311 μM
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 404.3 화학식

C19H12F4N4O2

 보관 (수령일로부터)
CAS 번호 745833-23-2 SDF 다운로드 원액 보관

동의어 N/A Smiles C1=CC(=C(C(=C1)F)N(C2=NC(=C(C=C2)C(=O)N)C3=C(C=C(C=C3)F)F)C(=O)N)F

용해도

In vitro
배치:

DMSO : 81 mg/mL (200.34 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

특징
Highly selective, orally active inhibitor of p38 MAPK.
Targets/IC50/Ki
p38α
(Cell-free assay)
4 nM-20 nM
시험관 내(In vitro)

혈소판을 VX-702 (1 μM)로 전처리하면 트롬빈, SFLLRN, AYPGKF, U46619 및 콜라겐을 포함한 혈소판 작용제에 의해 유도되는 p38 활성화(IC50 4~20 nM)가 완전히 또는 부분적으로 억제됩니다. 이 화합물은 항혈소판 요법의 유무에 관계없이 p38 MAPK 작용제 중 어느 것에 의해서도 유도되는 혈소판 응집에 영향을 미치지 않습니다. 이는 용량 의존적으로 IL-6, IL-1β 및 TNFα의 생성을 억제합니다 (각각 IC50 = 59, 122 및 99 ng/mL).

생체 내(In vivo)

VX-702의 반감기는 16~20시간이며, 중앙 청소율은 3.75 L/h, 분포 용적은 73 L/kg입니다. 이 화합물의 AUC 및 Cmax 값은 모두 용량 비례하며, 주로 신장으로 제거됩니다. 이 화합물 (0.1 mg/kg 1일 2회 용량)은 동등한 효과를 나타냅니다. 또한 이 화학 물질 (5 mg/kg 1일 2회)은 손목 관절 침식 및 염증 점수의 백분율 억제로 측정됩니다. 허혈 후 p38 MAPK 활성화를 선택적으로 억제하며 ERKs 및 JNKs에는 영향을 미치지 않습니다. MI/AAR 비율은 5 mg/kg 및 비히클 그룹에 비해 50 mg/kg 그룹에서 유의하게 감소합니다.
참조
  • [4] http://circ.ahajournals.org/content/108/17.toc

임상시험 정보

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

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT00395577 Completed
Rheumatoid Arthritis
Vertex Pharmaceuticals Incorporated
 November 2006 Phase 2

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