INCB018424 (Ruxolitinib)

Catalog No. A11041

INCB018424 (Ruxolitinib)是有效和选择性的Janus相关激酶JAK1/2抑制剂，对JAK1，JAK2和JAK3的IC50分别为2.7、4.5和332 nM。

Product Citations

Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
Rasmus Siersbek, .et al. IL6/STAT3 Signaling Hijacks Estrogen Receptor α Enhancers to Drive Breast Cancer Metastasis, Cancer cell, 2020, Jul 6;S1535-6108(20)30311-1 PMID: 32679107
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
Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
Kagoya Y, .et al. JAK2V617F+ myeloproliferative neoplasm clones evoke paracrine DNA damage to adjacent normal cells through secretion of lipocalin-2., Blood., 2014, Nov 6;124(19):2996-3006 PMID: 25217696

Technical details

Catalog Num	A11041
M. Wt	306.4
Formula	C17H18N6
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	941678-49-5
Synonyms	Ruxolitinib, INCB18424
SMILES	C1CCC(C1)[C@@H](CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3

Biological Activity

INCB018424 (Ruxolitinib)是有效和选择性的Janus相关激酶JAK1/2抑制剂，对JAK1，JAK2和JAK3的IC50分别为2.7、4.5和332 nM。

Solubility *

In vitro (25°C)	DMSO	59 mg/mL (192.57 mM)
	Water	Insoluble
	Ethanol	59 mg/mL (192.57 mM)
In vivo	2% DMSO+30% PEG 300+ddH2O	4 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	32.64 mL	163.19 mL	326.37 mL
0.5 mM	6.53 mL	32.64 mL	65.27 mL
1 mM	3.26 mL	16.32 mL	32.64 mL
5 mM	0.65 mL	3.26 mL	6.53 mL

*The above data is based on the productmolecular weight 306.4 . 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.