CP-690550 (Tofacitinib citrate)

Catalog No. A10241

CP-690550 (Tofacitinib citrate)是口服的高选择性Janus激酶（JAK）酶抑制剂。

Product Citations

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

Technical details

Catalog Num	A10241
M. Wt	504.5
Formula	C16H20N6O.C6H8O7
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	540737-29-9
Synonyms	CP690550, tasocitinib citrate, CP-690,550
SMILES	C[C@@H]1CCN(C[C@@H]1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

Biological Activity

CP-690550 (Tofacitinib citrate)是口服的高选择性Janus激酶（JAK）酶抑制剂。

Targets

Target	Value
JAK3	IC50: 1nM
JAK2	IC50: 20nM
JAK1	IC50: 112nM
ROCK2	IC50: 3.4μM
LCK	IC50: 3.87μM
IRK	IC50: >10μM
CDK2	IC50: >10μM
CDK5	IC50: >10μM
EGFR	IC50: >10μM
MAPK2/ERK2	IC50: >10μM
JNK1/SAPK1c	IC50: >10μM
SAPK2a/p38	IC50: >10μM
SAPK2b/p38b2	IC50: >10μM
SAPK3/p38g	IC50: >10μM
SAPK4/p38d	IC50: >10μM
MAPKAPK2	IC50: >10μM
MAPKAP-K1b	IC50: >10μM
MSK1	IC50: >10μM
PRAK	IC50: >10μM
PKA	IC50: >10μM
PKCα	IC50: >10μM
PDK-1	IC50: >10μM
PKBα	IC50: >10μM
SGK	IC50: >10μM
p70S6K	IC50: >10μM
GSK-3β	IC50: >10μM
AMPK	IC50: >10μM
Chk1	IC50: >10μM
CK2	IC50: >10μM
PHK	IC50: >10μM
CSK	IC50: >10μM
CDK2/CyclinA	IC50: >10μM
PI3K	IC50: >10μM

Solubility *

In vitro (25°C)	DMSO	Warmed: 94 mg/mL (186.32 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	0.5% methylcellulose	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	19.82 mL	99.11 mL	198.22 mL
0.5 mM	3.96 mL	19.82 mL	39.64 mL
1 mM	1.98 mL	9.91 mL	19.82 mL
5 mM	0.4 mL	1.98 mL	3.96 mL

*The above data is based on the productmolecular weight 504.5 . 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.