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Sunitinib (SU11248) - Moligand™, 10mM in DMSO , Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of fms related receptor tyrosine kinase 4;Inhibitor of kinase insert domain receptor;Inhibitor o, Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of fms related receptor tyrosine kinase 4;Inhibitor of kinase insert domain receptor;Inhibitor of KIT proto-oncogene; receptor tyrosine kinase;I

CAS: 557795-19-4 Cat. No.: S408232 분자식: C22H27FN4O2 분자량: 398.47 EC 번호: 111-194-2 PubChem CID: 5329102
19 Citations COA
Sunitinib (SU11248) - Moligand™, 10mM in DMSO CAS No(557795-19-4) by Aladdin Scientific
주문 가능
등급 & 순도 Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools. 10mM in DMSO
Synonyms
(Z)-N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
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크기
USA
독일 (EU)*
가격
수량
1ml
S408232-1ml
1 재고 있음
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US$33.90

US$49.90
저장 US$16.00 (32.06%)
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벌크 / 맞춤
♡ 위시 리스트 ⇅ 비교하기에 추가 ⎙ 페이지 인쇄
SDS
Safety data
COA
Certificate
DS
데이터시트
SP
사양서
개요 사양 이름과 식별자 문서 고급 데이터 관련 대상(인간) 인증서(CoA, COO, BSE/TSE 및 분석 차트) 화학 및 물리적 특성 Citations of This Product 솔루션 계산기 리뷰
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이 등급을 선택하는 이유

Moligand™, 10mM in DMSO Moligand™ 최소한의 기준선 간섭이 필요한 민감한 크로마토그래피 및 분석 워크플로우용.

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보관 및 배송

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품질 문서

SDS, COA, 데이터시트, 사양서를 다운로드할 수 있습니다. 로트별 COA는 로트 번호 조회를 통해 확인할 수 있습니다.

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문헌적 근거

크로마토그래피, 유기 합성 및 교차 커플링 반응 분야의 동료 심사 논문 19편에서 인용되었습니다.

개요

Information

Sunitinib (SU11248) is a multi-targeted RTK inhibitor targetingVEGFR2(Flk-1) andPDGFRβwithIC50of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity ofIRE1α. Sunitinib inducesautophagya
In vitro

Sunitinib also potently inhibits Kit and FLT-3. Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner.

In vivo

Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model.
Cell Data

cell lines：

Concentrations：Dissolved in DMSO, final concentrations ~10 μM

Incubation Time：24 and 48 hours

Powder Purity:≥99%

사양

동의어
(Z)-N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide
사양 및 순도
Moligand™, 10mM in DMSO
생화학 및 생리적 메커니즘
Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces au
보관 조건
Store at -80°C
배송
Dry ice packs + Cold packs
이 제품은 콜드 체인 배송이 필요합니다.지상 및 기타 경제 서비스는 사용할 수 없습니다.
등급
Moligand™
작업 유형
INHIBITOR
작동 메커니즘
Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of fms related receptor tyrosine kinase 4;Inhibitor of kinase insert domain receptor;Inhibitor of KIT proto-oncogene; receptor tyrosine kinase;I
이름과 식별자
이성체 SMILES
CCN(CC)CCNC(=O)C1=C(NC(=C1C)/C=C\2/C3=C(C=CC(=C3)F)NC2=O)C
PubChem CID
5329102
UN 번호
2811
포장 그룹
III
분자량
398.47

문서

📋 안전 데이터 시트(SDS)

위험성, 취급, 보관 및 규제 준수를 포괄하는 종합 문서.

<<<<<<< HEAD SDS 다운로드 → ======= SDS 다운로드 → >>>>>>> release248-p3

✅ 분석 성적서(COA)

로트별 품질 데이터. 로트 번호를 입력하여 정확한 COA를 확인하세요.

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📊 데이터시트

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🔬 사양서

이 등급의 전체 품질 특성 및 합격 기준.

사양서 보기 →

고급 데이터

관련 대상(인간)
GJD4 Tdark Gap junction delta-4 protein (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DLK1 Tchem Protein delta homolog 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CSF1R Tclin Macrophage colony-stimulating factor 1 receptor (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DAPK3 Tchem Death-associated protein kinase 3 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret (11 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK17A Tchem Serine/threonine-protein kinase 17A (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK10 Tchem Serine/threonine-protein kinase 10 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK33 Tchem Serine/threonine-protein kinase 33 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK4 Tchem Serine/threonine-protein kinase 4 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FLT4 Tclin Vascular endothelial growth factor receptor 3 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
IRAK1 Tchem Interleukin-1 receptor-associated kinase 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (38 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GAK Tchem Cyclin-G-associated kinase (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FGFR1 Tclin Fibroblast growth factor receptor 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CSNK1D Tchem Casein kinase I isoform delta (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ITK Tclin Tyrosine-protein kinase ITK/TSK (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MERTK Tchem Tyrosine-protein kinase Mer (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TNIK Tchem TRAF2 and NCK-interacting protein kinase (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PDGFRA Tclin Platelet-derived growth factor receptor alpha (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PHKG1 Tchem Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PDGFRB Tclin Platelet-derived growth factor receptor beta (15 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MINK1 Tchem Misshapen-like kinase 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RPS6KA2 Tchem Ribosomal protein S6 kinase alpha-2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP3K19 Tchem Mitogen-activated protein kinase kinase kinase 19 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
LCK Tclin Tyrosine-protein kinase Lck (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP4K1 Tchem Mitogen-activated protein kinase kinase kinase kinase 1 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
LRRK2 Tchem Leucine-rich repeat serine/threonine-protein kinase 2 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK1 Tclin Tyrosine-protein kinase JAK1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BMP2K Tchem BMP-2-inducible protein kinase (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Tchem Uncharacterized protein FLJ45252 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FLT1 Tclin Vascular endothelial growth factor receptor 1 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (33 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
AAK1 Tchem AP2-associated protein kinase 1 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PRKAA1 Tclin 5'-AMP-activated protein kinase catalytic subunit alpha-1 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
AXL Tchem Tyrosine-protein kinase receptor UFO (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ULK1 Tchem Serine/threonine-protein kinase ULK1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ULK2 Tchem Serine/threonine-protein kinase ULK2 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CLK1 Tchem Dual specificity protein kinase CLK1 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CLK2 Tchem Dual specificity protein kinase CLK2 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CLK4 Tchem Dual specificity protein kinase CLK4 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KIT Tclin Mast/stem cell growth factor receptor Kit (27 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PAK3 Tchem Serine/threonine-protein kinase PAK 3 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MYLK3 Tchem Myosin light chain kinase 3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MYLK Tchem Myosin light chain kinase, smooth muscle (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
인증서(CoA, COO, BSE/TSE 및 분석 차트)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
화학 및 물리적 특성
용해성Solubility (25°C) In vitro Ethanol: 49 mg/mL (196.98 mM); Water: 21 mg/mL (84.42 mM); DMSO: 12 mg/mL (48.24 mM);
Citations of This Product
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