Sorafenib Tosylate (Nexavar)

Catalog No. A10001

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。

Product Citations

Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
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
Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
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Technical details

Catalog Num	A10001
M. Wt	637
Formula	C21H16ClF3N4O3.C7H8O3S
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	475207-59-1
Synonyms	Bay 43-9006
SMILES	CC1=CC=C(C=C1)S(=O)(=O)O.CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F

Biological Activity

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。

Targets

Target	Value
Raf-1	IC50: 6nM
VEGFR2/Flk1	IC50: 15nM
B-Raf	IC50: 22nM
B-Raf(V599E)	IC50: 38nM
PDGFRβ	IC50: 57nM
mPDGFRβ	IC50: 57nM
FLT3	IC50: 58nM
c-Kit	IC50: 68nM
VEGFR2	IC50: 90nM
FGFR1	IC50: 580nM
ERK1	IC50: >10μM
MEK1	IC50: >10μM
EGFR	IC50: >10μM
HER2	IC50: >10μM
IGF-1R	IC50: >10μM
c-Met	IC50: >10μM
PKB	IC50: >10μM
PKA	IC50: >10μM
CDK1/CyclinB	IC50: >10μM
PKCα	IC50: >10μM
PKCγ	IC50: >10μM
Pim1	IC50: >10μM

Solubility *

In vitro (25°C)	DMSO	114 mg/mL (178.95 mM)
	Water	<1 mg/mL
	Ethanol	Insoluble
In vivo	2% Cremophor EL, 2% N,N-dimethylacetamide	28 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	15.7 mL	78.49 mL	156.99 mL
0.5 mM	3.14 mL	15.7 mL	31.4 mL
1 mM	1.57 mL	7.85 mL	15.7 mL
5 mM	0.31 mL	1.57 mL	3.14 mL

*The above data is based on the productmolecular weight 637. 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.