Tafetinib
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 96.20%
- CAS No.: 1032265-57-8
- Formula: C24H29FN4O2
- Molecular Weight:424.51
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
All VEGFR Isoforms
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Biological Activity
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Cell Line
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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] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1032265-57-8
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Appearance Solid
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Molecular Weight 424.51
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Formula C24H29FN4O2
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Color Light yellow to yellow
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SMILES
CCN(CC)CCNC(C1=C(C)NC2=C1CCC/C2=C3C(NC4=CC=C(F)C=C/34)=O)=O
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Synonyms
SIM010603
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : < 1 mg/mL (insoluble or slightly soluble)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 1% CMC-Na/saline water
Solubility: 10 mg/mL (23.56 mM); Suspended solution; Need ultrasonic
Purity & Documentation
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Data Sheet (268 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)