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A4013012

Sunitinib Malate , ≥99% , 341031-54-7

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

Pack Size Price Stock Quantity
100MG RMB84.80 In Stock
500MG RMB151.20 In Stock
1G RMB265.60 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: 189-191°C
storage temp.  room temp
solubility  DMSO: >10mg/mL
form  powder
color  Orange
Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChIKey XGQXULJHBWKUJY-LYIKAWCPSA-N
SMILES [C@@H](O)(C(=O)O)CC(=O)O.C(/C1NC(C)=C(C(=O)NCCN(CC)CC)C=1C)=C1/C(NC2=CC=C(F)C=C/12)=O |&1:0,r|

Description and Uses

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.

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.

Safety

Symbol(GHS) 
GHS08
Signal word  Danger
Hazard statements  H360-H372
Precautionary statements  P201-P308+P313
Hazard Codes  T
Risk Statements  61-2-48/25-36/37-22-53
Safety Statements  53-22-36/37-24/25
WGK Germany  2
HS Code  29337900

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