Sunitinib Malate
Synonym(s):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
- CAS NO.:341031-54-7
- Empirical Formula: C26H33FN4O7
- Molecular Weight: 532.57
- MDL number: MFCD08282795
- EINECS: 638-825-9
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-12-20 13:21:23
What is Sunitinib Malate?
Description
Sunitinib is a small molecule inhibitor of receptor tyrosine kinases, including FLK1 (Ki = 9 nM), PDGFRβ (Ki = 8 nM), and FLT3. It is at least 10-fold selective for FLK1 and PDGFRβ over a variety of tyrosine kinases in a panel, including EGFR, Cdk2, Met, IGFR-1, Abl, and Src. Sunitinib inhibits VEGF-dependent FLK1 and PDGF-dependent PDGFRβ phosphorylation (IC50s = 10 and 10 nM, respectively) as well as phosphorylation of FLT3 and FLT3 carrying the activating internal tandem duplication mutation (FLT3-ITD; IC50s = 250 and 50 nM, respectively). It decreases VEGF- and FGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50s = 30 and 700 nM, respectively) and reduces tumor growth in a variety of mouse xenograft models when administered at doses ranging from 20 to 80 mg/kg per day. Formulations containing sunitinib have been used in the treatment of gastrointestinal stromal tumors and metastatic renal cell carcinoma.
The Uses of Sunitinib Malate
Sunitinib Malate (Sutent, 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.
What are the applications of Application
Sunitinib Malate is an antineoplastic agent, Flk-1 inhibitor, and ATP-competitve inhibitor of PDGFRβ
Properties of Sunitinib Malate
Melting point: | 189-191°C |
storage temp. | room temp |
solubility | DMSO: >10mg/mL |
form | powder |
color | Orange |
Safety information for Sunitinib Malate
Signal word | Danger |
Pictogram(s) |
Health Hazard GHS08 |
GHS Hazard Statements |
H360:Reproductive toxicity H372:Specific target organ toxicity, repeated exposure |
Precautionary Statement Codes |
P201:Obtain special instructions before use. P308+P313:IF exposed or concerned: Get medical advice/attention. |
Computed Descriptors for Sunitinib Malate
InChIKey | XGQXULJHBWKUJY-LYIKAWCPSA-N |
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