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 分子式: C₂₂H₂₇FN₄O₂ 分子量: 398.47 EC番号: 111-194-2 PubChem CID: 5329102

グレード＆純度 Moligand™, 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

概要

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 K_i 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%

仕様

同義語

(Z)-N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

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

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

INHIBITOR

作用メカニズム

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

名前と識別子

異性体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番号

2811

包装グループ

III

分子量

398.47

関連ターゲット（人間）

GJD4 Tdark Gap junction delta-4 protein (0 Activities)

Discover Target: GJD4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DLK1 Tchem Protein delta homolog 1 (2 Activities)

Discover Target: DLK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CSF1R Tclin Macrophage colony-stimulating factor 1 receptor (3 Activities)

Discover Target: CSF1R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DAPK3 Tchem Death-associated protein kinase 3 (3 Activities)

Discover Target: DAPK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret (11 Activities)

Discover Target: RET

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

STK17A Tchem Serine/threonine-protein kinase 17A (5 Activities)

Discover Target: STK17A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

STK10 Tchem Serine/threonine-protein kinase 10 (3 Activities)

Discover Target: STK10

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

STK33 Tchem Serine/threonine-protein kinase 33 (3 Activities)

Discover Target: STK33

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

STK4 Tchem Serine/threonine-protein kinase 4 (3 Activities)

Discover Target: STK4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT4 Tclin Vascular endothelial growth factor receptor 3 (3 Activities)

Discover Target: FLT4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

IRAK1 Tchem Interleukin-1 receptor-associated kinase 1 (2 Activities)

Discover Target: IRAK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (38 Activities)

Discover Target: FLT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GAK Tchem Cyclin-G-associated kinase (3 Activities)

Discover Target: GAK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR1 Tclin Fibroblast growth factor receptor 1 (1 Activities)

Discover Target: FGFR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta (3 Activities)

Discover Target: CSNK1D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ITK Tclin Tyrosine-protein kinase ITK/TSK (3 Activities)

Discover Target: ITK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MERTK Tchem Tyrosine-protein kinase Mer (3 Activities)

Discover Target: MERTK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TNIK Tchem TRAF2 and NCK-interacting protein kinase (6 Activities)

Discover Target: TNIK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha (4 Activities)

Discover Target: PDGFRA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PHKG1 Tchem Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (3 Activities)

Discover Target: PHKG1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRB Tclin Platelet-derived growth factor receptor beta (15 Activities)

Discover Target: PDGFRB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MINK1 Tchem Misshapen-like kinase 1 (2 Activities)

Discover Target: MINK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RPS6KA2 Tchem Ribosomal protein S6 kinase alpha-2 (3 Activities)

Discover Target: RPS6KA2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP3K19 Tchem Mitogen-activated protein kinase kinase kinase 19 (2 Activities)

Discover Target: MAP3K19

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

LCK Tclin Tyrosine-protein kinase Lck (1 Activities)

Discover Target: LCK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP4K1 Tchem Mitogen-activated protein kinase kinase kinase kinase 1 (3 Activities)

Discover Target: MAP4K1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

LRRK2 Tchem Leucine-rich repeat serine/threonine-protein kinase 2 (2 Activities)

Discover Target: LRRK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

JAK1 Tclin Tyrosine-protein kinase JAK1 (2 Activities)

Discover Target: JAK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BMP2K Tchem BMP-2-inducible protein kinase (3 Activities)

Discover Target: BMP2K

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Tchem Uncharacterized protein FLJ45252 (1 Activities)

Explore this target

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT1 Tclin Vascular endothelial growth factor receptor 1 (5 Activities)

Discover Target: FLT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 (33 Activities)

Discover Target: KDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AAK1 Tchem AP2-associated protein kinase 1 (4 Activities)

Discover Target: AAK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKAA1 Tclin 5'-AMP-activated protein kinase catalytic subunit alpha-1 (3 Activities)

Discover Target: PRKAA1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHEK2 Tchem Serine/threonine-protein kinase Chk2 (3 Activities)

Discover Target: CHEK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AXL Tchem Tyrosine-protein kinase receptor UFO (5 Activities)

Discover Target: AXL

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ULK1 Tchem Serine/threonine-protein kinase ULK1 (2 Activities)

Discover Target: ULK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ULK2 Tchem Serine/threonine-protein kinase ULK2 (2 Activities)

Discover Target: ULK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK1 Tchem Dual specificity protein kinase CLK1 (4 Activities)

Discover Target: CLK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK2 Tchem Dual specificity protein kinase CLK2 (4 Activities)

Discover Target: CLK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK4 Tchem Dual specificity protein kinase CLK4 (4 Activities)

Discover Target: CLK4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit (27 Activities)

Discover Target: KIT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (5 Activities)

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PAK3 Tchem Serine/threonine-protein kinase PAK 3 (3 Activities)

Discover Target: PAK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MYLK3 Tchem Myosin light chain kinase 3 (1 Activities)

Discover Target: MYLK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MYLK Tchem Myosin light chain kinase, smooth muscle (1 Activities)

Discover Target: MYLK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

化学的性質と物理的性質

• 溶解度: Solubility (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)