SML2274

DDR1-IN-1

Name: DDR1-IN-1
Brand: SIGMA

≥98% (HPLC)

동의어(들):

4-((4-Ethylpiperazin-1-yl)methyl)-N-(4-methyl-3-(2-oxoindolin-5-yloxy)phenyl)-3-(trifluoromethyl)benzamide, N-[3-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)oxy]-4-methylphenyl]-4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)benzamide

조직 및 계약 가격을 보려면 로그인를 클릭합니다.

크기 선택

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):

C₃₀H₃₁F₃N₄O₃

CAS 번호:

1449685-96-4

Molecular Weight:

552.59

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD28144507

Assay:

≥98% (HPLC)

Form:

powder

주요 문서

모든 문서 보기

기술 서비스

도움이 필요하신가요? 저희 숙련된 과학자 팀이 도와드리겠습니다.

도움 문의

기술 서비스

도움이 필요하신가요? 저희 숙련된 과학자 팀이 도와드리겠습니다.

도움 문의

InChI

1S/C30H31F3N4O3/c1-3-36-10-12-37(13-11-36)18-21-6-5-20(15-25(21)30(31,32)33)29(39)34-23-7-4-19(2)27(17-23)40-24-8-9-26-22(14-24)16-28(38)35-26/h4-9,14-15,17H,3,10-13,16,18H2,1-2H3,(H,34,39)(H,35,38)

SMILES string

CC(C=CC(NC(C1=CC(C(F)(F)F)=C(CN2CCN(CC)CC2)C=C1)=O)=C3)=C3OC4=CC(CC(N5)=O)=C5C=C4

InChI key

AOZPVMOOEJAZGK-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

DDR1-IN-1 is a type II, subtype-selective discoidin domain receptor (DDR) tyrosine kinase inhibitor (DDR1/2 IC50 = 105 nM/413 nM) that effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC50 = 86.76 nM) with excellent selectivity over a panel of >380 kinases. DDR1-IN-1 inhibits DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) upon collagen stimulation (IC50 < 2.5 μM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture (123%, 70%, 50% of control, respectively, post 48-hr 250 nM DDR1-IN-1, 82.5 nM GSK2126458, or combined treatment).

DDR1-IN-1 protects cells from apoptosis by inhibiting collagen-mediated Bcl-2-interacting killer (BIK) induction at both mRNA and protein levels.

Potent, selective, type II tyrosine kinase inhibitor against discoidin domain receptor DDR1/2.

저장 등급

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

가장 최신 버전 중 하나를 선택하세요:

시험 성적서(COA)

Lot/Batch Number

It looks like we've run into a problem, but you can still download Certificates of Analysis from our 문서 section.

도움이 필요하시면 연락하세요. 고객 지원 부서

이 제품을 이미 가지고 계십니까?

문서 라이브러리에서 최근에 구매한 제품에 대한 문서를 찾아보세요.

문서 라이브러리 방문

Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.

Hyung-Gu Kim et al.

ACS chemical biology, 8(10), 2145-2150 (2013-08-01)

The DDR1 receptor tyrosine kinase is activated by matrix collagens and has been implicated in numerous cellular functions such as proliferation, differentiation, adhesion, migration, and invasion. Here we report the discovery of a potent and selective DDR1 inhibitor, DDR1-IN-1, and

Mechanotransduction-modulated fibrotic microniches reveal the contribution of angiogenesis in liver fibrosis.

Longwei Liu et al.

Nature materials, 16(12), 1252-1261 (2017-11-25)

The role of pathological angiogenesis on liver fibrogenesis is still unknown. Here, we developed fibrotic microniches (FμNs) that recapitulate the interaction of liver sinusoid endothelial cells (LSECs) and hepatic stellate cells (HSCs). We investigated how the mechanical properties of their

A membrane-type-1 matrix metalloproteinase (MT1-MMP)-discoidin domain receptor 1 axis regulates collagen-induced apoptosis in breast cancer cells.

Delphine Assent et al.

PloS one, 10(3), e0116006-e0116006 (2015-03-17)

During tumour dissemination, invading breast carcinoma cells become confronted with a reactive stroma, a type I collagen-rich environment endowed with anti-proliferative and pro-apoptotic properties. To develop metastatic capabilities, tumour cells must acquire the capacity to cope with this novel microenvironment.

Ultra-deep tyrosine phosphoproteomics enabled by a phosphotyrosine superbinder.

Yangyang Bian et al.

Nature chemical biology, 12(11), 959-966 (2016-10-19)

We present a new strategy for systematic identification of phosphotyrosine (pTyr) by affinity purification mass spectrometry (AP-MS) using a Src homology 2 (SH2)-domain-derived pTyr superbinder as the affinity reagent. The superbinder allows for markedly deeper coverage of the Tyr phosphoproteome

A Membrane-Type-1 Matrix Metalloproteinase (MT1-MMP) - Discoidin Domain Receptor 1 Axis Regulates Collagen-Induced Apoptosis in Breast Cancer Cells

Assent D, et al.

PLoS ONE, 10, e0116006-e0116006 (2015)

모든 관련된 서류 보기

자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..

고객지원팀으로 연락바랍니다.

DDR1-IN-1

≥98% (HPLC)

크기 선택

제품정보 (DICE 배송 시 비용 별도)

주요 문서

속성

InChI

SMILES string

InChI key

assay

form

color

solubility

storage temp.

관련 카테고리

설명

Biochem/physiol Actions

안전성 정보

저장 등급

wgk

flash_point_f

flash_point_c

문서

시험 성적서(COA)

이 제품을 이미 가지고 계십니까?

관련 참고 논문

기술 서비스