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Ruxolitinib Phosphate (INC-424, INCB-18424, INCB-018424, Jakafi and Jakavi)

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Ruxolitinib Phosphate (INC-424, INCB-18424, INCB-018424, Jakafi and Jakavi)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
500mg$380In Stock
1g$560In Stock
5g$1415In Stock

Cat #: V0076 CAS #: 1092939-17-7 Purity ≥ 98%

Description: Ruxolitinib Phosphate (Jakafi and Jakavi), the phosphate salt of ruxolitinib which is also known as INC424, INCB18424 or INCB018424, is a first-in class, potent, selective, and orally bioavailable JAK1/2 (Janus-associated kinase) inhibitor with IC50 of 3.3 nM/2.8 nM in cell-free assays, it exhibits >130-fold selectivity for JAK1/2 versus JAK3.

References: Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117.

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Molecular Weight (MW)404.36
Molecular FormulaC₁₇H₂₁N₆O₄P
CAS No.1092939-17-7
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 61 mg/mL (199.1 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo2% DMSO+30% PEG 300+ddH2O: 5 mg/mL
SMILES CodeN#CC[C@@H](N1N=CC(C2=C3C(NC=C3)=NC=N2)=C1)C4CCCC4.O=P(O)(O)O
SynonymsINCB-018424 phosphate, INCB 018424, INCB018424; INC424, INC424, INC-424; INCB18424, INCB 18424, INCB-18424; Jakafi and Jakavi (trade name)
ProtocolIn VitroRuxolitinib (INCB018424) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation. Ruxolitinib inhibits the growth of HEL cells with EC50 of 186 nM. Ruxolitinib markedly increases apoptosis in Ba/F3-EpoR-JAK2V617F cell system, and inhibits hematopoietic progenitor cell proliferation in primary MPN patient samples.
In VivoRuxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cells without causing anemia or lymphopenia.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.4730 mL12.3652 mL24.7304 mL49.4609 mL
5mM0.4946 mL2.4730 mL4.9461 mL9.8922 mL
10mM0.2473 mL1.2365 mL2.4730 mL4.9461 mL
20mM0.1237 mL0.6183 mL1.2365 mL2.4730 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.