Sunitinib Malate

Catalog No. A10880

Sunitinib Malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，也会抑制c-Kit的活性。用于治疗肾细胞癌（RCC）和伊马替尼耐药的胃肠道间质瘤（GIST）。

Product Citations

Rachel K Toth, .et al. Stabilization of PIM Kinases in Hypoxia Is Mediated by the Deubiquitinase USP28, Cells, 2022, Mar 16;11(6):1006 PMID: 35326457
Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
Thibaut Fourniols, .et al. Inhibition of Colorectal Cancer-Associated Fibroblasts by Lipid Nanocapsules Loaded With Acriflavine or Paclitaxel, Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277

Technical details

Catalog Num	A10880
M. Wt	532.6
Formula	C22H27FN4O2.C4H6O5
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	341031-54-7
Synonyms	SU-11248
SMILES	CCN(CC)CCNC(=O)C1=C(NC(=C1C)/C=C\2/C3=C(C=CC(=C3)F)NC2=O)C.C([C@@H](C(=O)O)O)C(=O)O

Biological Activity

Targets

Target	Value
Kit
FLT3
PDGFRβ	IC50: 2nM
VEGFR2	IC50: 80nM
FGFR1	IC50: 2.9μM
EGFR	IC50: >20μM

Solubility *

In vitro (25°C)	DMSO	13 mg/mL (24.41 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	4% DMSO+30% PEG 300+ddH2O	1 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	18.78 mL	93.88 mL	187.76 mL
0.5 mM	3.76 mL	18.78 mL	37.55 mL
1 mM	1.88 mL	9.39 mL	18.78 mL
5 mM	0.38 mL	1.88 mL	3.76 mL

*The above data is based on the productmolecular weight 532.6 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.