Tofacitinib (CP690550; tasocitinib)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
500mg	$300	In Stock
1g	$500	In Stock
5g	$1265	In Stock

: [email protected] [email protected]

Cat #: V0342 CAS #: 477600-75-2 (free base) Purity ≥ 98%

Description: Tofacitinib (also known as tasocitinib or CP-690550, sold under the brand Xeljanz), is a novel and potent inhibitor of JAK3 (Janus-Associated kinase) with potential anti-inflammatory activity.

References: Jiang JK, et al. Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). J Med Chem. 2008 Dec 25;51(24):8012-8.

Top Publications Citing Invivochem Products

Product Catalog 2022

Guide to Product Handling

Publications Citing InvivoChem Products

Product Promise

Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	312.37
Molecular Formula	C16H20N6O
CAS No.	477600-75-2 (free base)
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 62 mg/mL (198.5 mM)r
	Water: <1 mg/mLr
	Ethanol: <1 mg/mL
Solubility In Vivo	30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
SMILES Code	N#CCC(N1C[C@H](N(C)C2=C3C(NC=C3)=NC=N2)[C@H](C)CC1)=O
Synonyms	CP-690550; CP690550; CP 690550; Tasocitinib; Tofacitinib; Xeljanz (Trade name); Tofacitinib free base;

Protocol	In Vitro	Tofacitinib (CP-690550) citrate binds potentially at JAK3 and JAK2 as 2.2 nM and 5 nM (Kd). The report includes additional binding for Tofacitinib at Camk1 (Kd of 5,000 nM), DCamkL3 (Kd of 4.5 nM), Mst2 (Kd of 4,300 nM), Pkn1 (Kd of 200 nM), Rps6ka2 (Kin.Dom.2-C-terminal) (Kd of 1,400 nM), Rps6ka6 (Kin.Dom.2-C-terminal) (Kd of 1,200 nM), Snark (Kd of 420 nM), Tnk1 (Kd of 640 nM) and Tyk2 (Kd of 620 nM).
Protocol	In Vivo	Animals that are treated with Tofacitinib show a significantly lower production of anti-drug antibodies (ADAs) compare with PEG-treated control mice (for five weeks after initial immunization, p<0.01, n=8). Moreover ADAs become detectable earliest on day 28. A difference of 1000- to 200-fold in titers to SS1P is apparent from days 21 through 35, respectively. Compare to SS1P, mice injected with keyhole limpet hemocyanin (KLH) generate a more rapid antibody response. Yet, the administration of Tofacitinib reduces anti-KLH titers compare to controls (p<0.05 on day 21, p<0.01 on day 28, respectively, n=5). Reductions in titers ranged from 5000- to 250-fold from days 21 through 28, respectively.

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	1mg	5mg	10mg	20mg
1mM	3.2013 mL	16.0067 mL	32.0133 mL	64.0266 mL
5mM	0.6403 mL	3.2013 mL	6.4027 mL	12.8053 mL
10mM	0.3201 mL	1.6007 mL	3.2013 mL	6.4027 mL
20mM	0.1601 mL	0.8003 mL	1.6007 mL	3.2013 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

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)

Volume_(start)

Concentration_(final)

Volume_(final)

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.