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Ruxolitinib (INCB18424) JAK1/2 inhibitor

Cat.No.S1378

Ruxolitinib (INCB18424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. This compound kills tumor cells through toxic mitophagy. It induces autophagy and enhances apoptosis.

Ruxolitinib (INCB18424) JAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 306.37

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	EGFR STAT Pim
Other JAK Inhibitors	BMS-986165 (Deucravacitinib) AZD1480 WP1066 Filgotinib (GLPG0634) Momelotinib (CYT387) AT9283 Gandotinib (LY2784544) Pacritinib (SB1518) NVP-BSK805 2HCl TG101209

Q&A of Ruxolitinib (INCB18424): Insights Rooted in Extensive Publications, Every Answer Cited

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Solubility in DMSO or Water

In vitro
Batch:

DMSO : 300 mg/mL (979.2 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 300 mg/mL (979.2 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 61 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 61 mg/mL (199.1 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 30 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 61 mg/mL (199.1 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 61 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 61 mg/mL (199.1 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 61 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (9.79mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; then continue Add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (9.79mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/mL clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Read more about Ruxolitinib (INCB18424) solubility in DMSO or water

Search directly for a cell line, or select a cell line to find matched working concentrations

Read more about Ruxolitinib (INCB18424) working concentrations for cell culture treatment

Ruxolitinib (INCB18424) is a potent inhibitor of JAK (0.40 nM), JAK2 (2.8 nM), JAK1 (3.3 nM), pSTAT3 (5.73 nM), TYK2 (19 nM), JAK3 (428 nM), STAT signaling (< 100 nM), ACVR1 (6100 nM), STAT1, STAT3, STAT4, STAT5, IL6, TNF, IFNG, PAD4, ACE2, ERK1, ERK2, NRAS, KRAS, PTPN11, CALR, MPL, SH2B3, IL2, IL4, IL7, IL15, IL21. Ruxolitinib (INCB18424) exhibits the greatest inhibitory potency toward JAK (IC50 = 0.40 nM).

Read more about selectivity & specificity

Mechanism of Action

Information	Ruxolitinib (INCB18424) is a potent, selective, ATP-competitive JAK1/2 inhibitor. It affects the JAK/STAT signaling pathway by binding to the JAK ATP-binding site and blocking STAT phosphorylation, inhibiting cell proliferation and inflammation, and promoting apoptosis.
Read more about Ruxolitinib (INCB18424) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about Ruxolitinib (INCB18424) Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	306.37	Formula	C₁₇H₁₈N₆	Storage (From the date of receipt)	3 years-20°C(in the dark) powder
CAS No.	941678-49-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	INCB018424			Smiles	C1CCC(C1)C(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3

Read more about storage & stability

Read more comparative analysis about Ruxolitinib (INCB18424)

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
What is the difference between S2902 and S1378 which seem to have same structure formula according to the product information?

Answer:
These two chemicals are the two different chiral forms of this compound. S2902 S-Ruxolitinib is the S form and S1378 Ruxolitinib is the D form. One of the carbon atoms in it is asymmetric, making the two molecules mirror images of each other. The biological activities of these two molecules can be very different because of the confirmation differences.

Question 2:
How about the half-life of this compound? How long is the duration of its inhibitory effect on JAK-STAT signaling?

Answer:
According to previous study, the half-life of this compound in body is about 2~3 hours. Generally, it is longer in vitro culture medium than in vivo. It was also used for 24 hours in paper. http://www.bloodjournal.org/cgi/pmidlookup?view=long&pmid=24711661.

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions

Concentration (start):

Dilution-folds:

Computed Result

C1=C0/X	C1:		LOG(C1):
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C3=C2/X	C3:		LOG(C3):
C4=C3/X	C4:		LOG(C4):
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C6=C5/X	C6:		LOG(C6):
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C8=C7/X	C8:		LOG(C8):