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Merck
CN

PZ0012

Sunitinib malate

≥98% (HPLC), powder, receptor tyrosine kinase inhibitor

别名:

N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-2-hydroxybutanedioic acid (1:1) salt, SU 011248, SU 11248, SU112248

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关于此项目

经验公式（希尔记法）:
C22H27FN4O2 · C4H6O5
化学文摘社编号:
341031-54-7
分子量:
532.56
UNSPSC Code:
12352200
PubChem Substance ID:
329823681
NACRES:
NA.77
MDL number:
MFCD08282795

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产品名称

Sunitinib malate, ≥98% (HPLC)

SMILES string

O[C@@H](CC(O)=O)C(O)=O.CCN(CC)CCNC(=O)c1c(C)[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c1C

InChI key

LBWFXVZLPYTWQI-IPOVEDGCSA-N

InChI

1S/C22H27FN4O2.C4H6O5/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28;5-2(4(8)9)1-3(6)7/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28);2,5H,1H2,(H,6,7)(H,8,9)/b17-12-;/t;2-/m.0/s1

assay

≥98% (HPLC)

form

powder

solubility

DMSO: >10 mg/mL

storage temp.

room temp

Quality Level

100

Gene Information

human ... CSF1R(1436), FLT1(2321), FLT3(2322), FLT4(2324), KDR(3791), KIT(3815), PDGFRA(5156), PDGFRB(5159), RET(5979)

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相关类别

Application

Sunitinib malate has been used:
  • to study its mechanism in the inhibition of MCF-7 cell migration and angiogenesis
  • as a reference molecule to compare its docking energies with other ligands/vascular endothelial growth factor receptor (VEGF) receptor blocker
  • used in proliferation assay

Biochem/physiol Actions

Sunitinib has greater bioavailability and potency compared to other inhibitors. It prevents angiogenesis.
Sunitinib malate is a receptor tyrosine kinase inhibitor, which targets VEGF-R1, VEGF-R2, VEGF-R3, PDGF-Rα, PDGF-Rβ, KIT, FLT3, CSF-1R, and RET. Sunitinib malate is an anticancer drug.

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

pictograms

Health hazard
GHS08

signalword

Danger

hcodes

H360,H372

Hazard Classifications

Repr. 1B - STOT RE 1 Oral

存储类别

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000338683
0000338683
030M4706V
0000058519
030M47063

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Nils Ohnesorge et al.
Frontiers in pharmacology, 10, 508-508 (2019-06-11)
Unbiased screening of large randomized chemical libraries in vivo is a powerful tool to find new drugs and targets. However, forward chemical screens in zebrafish can be time consuming and usually >99% of test compounds have no significant effect on
Sunitinib: from rational design to clinical efficacy
Chow LQM and Eckhardt SG
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 25(7), 884-896 (2007)
Iris Uribesalgo et al.
EMBO molecular medicine, 11(8), e9266-e9266 (2019-07-04)
Angiogenesis is a hallmark of cancer, promoting growth and metastasis. Anti-angiogenic treatment has limited efficacy due to therapy-induced blood vessel alterations, often followed by local hypoxia, tumor adaptation, progression, and metastasis. It is therefore paramount to overcome therapy-induced resistance. We
Sunitinib treatment inhibited human breast cancer cell migration through regulation furin interaction with substrates
Jin SJ, et al.
International Journal of Clinical and Experimental Medicine, 9(2), 2535-2541 (2016)
Kingkamon Junkunlo et al.
Stem cells and development, 26(20), 1449-1459 (2017-08-15)
The platelet-derived growth factor (PDGF) receptor, a tyrosine kinase (TK) receptor whose ligand is PDGF, is crucial in the transduction of extracellular signals into cells and mediates numerous processes, such as cell proliferation, differentiation, survival, and migration. We demonstrate the
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