2. Protein Tyrosine Kinase/RTK
  3. VEGFR RET c-Kit
  4. Tafetinib

Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis.

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Tafetinib Chemical Structure

Tafetinib Chemical Structure

CAS No. : 1032265-57-8

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Tafetinib Related Antibodies

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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Description

Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis[1].

Cellular Effect
Cell Line Type Value Description References
BXPC-3 IC50
0.52 μM
Compound: 22
Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay
[PMID: 23999040]
HepG2 IC50
7.27 μM
Compound: 22
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
[PMID: 23999040]
HT-29 IC50
1.2 μM
Compound: 22
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
[PMID: 23999040]
T-24 IC50
3.31 μM
Compound: 22
Antiproliferative activity against human T24 cells after 72 hrs by MTT assay
Antiproliferative activity against human T24 cells after 72 hrs by MTT assay
[PMID: 23999040]
Molecular Weight

424.51

Formula

C24H29FN4O2
CAS No.
SMILES

CCN(CC)CCNC(C1=C(C)NC2=C1CCC/C2=C3C(NC4=CC=C(F)C=C/34)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Tafetinib Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tafetinib1032265-57-8SIM010603SIM 010603SIM-010603VEGFRRETc-KitVascular endothelial growth factor receptorSCFRCD117SIM010603,Receptor tyrosine kinasesAnti-VEGFRAnti-PDGFRAngiogenesisInhibitorinhibitorinhibit

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