(3S,4R)-Tofacitinib - CAS 1092578-48-7
Catalog number: 1092578-48-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C16H20N6O
Molecular Weight:
312.37
COA:
Inquire
Targets:
JAK
Description:
Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
Synonyms:
CP-690550 citrate
MSDS:
Inquire
1.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).
Jiang JK1, Ghoreschi K, Deflorian F, Chen Z, Perreira M, Pesu M, Smith J, Nguyen DT, Liu EH, Leister W, Costanzi S, O'Shea JJ, Thomas CJ. J Med Chem. 2008 Dec 25;51(24):8012-8. doi: 10.1021/jm801142b.
Here, we examine the significance that stereochemistry plays within the clinically relevant Janus kinase 3 (Jak3) inhibitor 1 (CP-690,550). A synthesis of all four enantiopure stereoisomers of the drug was carried out and an examination of each compound revealed that only the enantiopure 3R,4R isomer was capable of blocking Stat5 phosphorylation (Jak3 dependent). Each compound was profiled across a panel of over 350 kinases, which revealed a high level of selectivity for the Jak family kinases for these related compounds. Each stereoisomer retained a degree of binding to Jak3 and Jak2 and the 3R,4S and 3S,4R stereoisomers were further revealed to have binding affinity for selected members of the STE7 and STE20 subfamily of kinases. Finally, an appraisal of the minimum energy conformation of each stereoisomer and molecular docking at Jak3 was performed in an effort to better understand each compounds selectivity and potency profiles.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related JAK Products


CAS 1257704-57-6 CEP33779

CEP33779
(CAS: 1257704-57-6)

CEP-33779 is a highly selective, orally active, small-molecule inhibitor of JAK2. CEP-33779 induced regression of established colorectal tumors, reduced angioge...

CAS 941685-37-6 Ruxolitinib S enantiomer

Ruxolitinib S enantiomer
(CAS: 941685-37-6)

Ruxolitinib S enantiomer, the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor to enter the clinic. It...

CAS 857064-38-1 WP1066

WP1066
(CAS: 857064-38-1)

WP1066 is a Stat3 inhibitor and JAK2 inhibitor. WP1066 is also a novel analogue of the JAK2 inhibitor AG490, in JAK2 V617F-positive erythroleukemia HEL cells a...

CAS 1187594-09-7 Baricitinib

Baricitinib
(CAS: 1187594-09-7)

Baricitinib is a selective and orally bioactive inhibitor of JAK1 and JAK2. Baricitinib inhibits intracellular signaling of multiple proinflammatory cytokines i...

CAS 944118-01-8 Peficitinib

Peficitinib
(CAS: 944118-01-8)

Peficitinib, also known as ASP015K and JNJ-54781532, is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in ...

CAS 1056636-07-7 CYT387 Mesylate

CYT387 Mesylate
(CAS: 1056636-07-7)

CYT387 Mesylate is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3.

CAS 1056634-68-4 Cyt387

Cyt387
(CAS: 1056634-68-4)

Cyt387, also called Momelotinib, under the IUPAC name N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide, is an ATP competitive inhib...

CAS 1092578-47-6 (3S,4S)-Tofacitinib

(3S,4S)-Tofacitinib
(CAS: 1092578-47-6)

Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.

CAS 1092939-17-7 Ruxolitinib phosphate

Ruxolitinib phosphate
(CAS: 1092939-17-7)

Ruxolitinib phosphate is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus J...

NS-018 hydrochloride
(CAS: 1239358-85-0)

The hydrochloride salt form of NS-018 which is a selective JAK2 as well as Src family tyrosine kinases inhibitor that could probably induce the apoptosis of tum...

CAS 1198300-79-6 Cerdulatinib

Cerdulatinib
(CAS: 1198300-79-6)

Cerdulatinib, also known as PRT2070 and PRT062070, is a novel, oral, dual spleen tyrosine kinase (Syk) and janus kinase (JAK) inhibitor. Cerdulatinib preferenti...

CAS 1206161-97-8 Filgotinib

Filgotinib
(CAS: 1206161-97-8)

Filgotinib, also known as GLPG0634, is a potent and selective JAK1 inhibitor. Filgotinib displayed a selectivity of 30-fold for JAK1- over JAK2-dependent signal...

CAS 477600-75-2 Tofacitinib

Tofacitinib
(CAS: 477600-75-2)

Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.It is currently approved f...

BMT-1438

BMT-1438 is a selective inhibitor of Janus kinase (JAK) family with less side effcts which is potentially used for the treatment of rheumatoid arthritis and oth...

BBT594
(CAS: 882405-89-2)

BBT594, also called as NVP-BBT594, a dihydroindole compound, originally developed as an inhibitor of wild-type and T315I-mutant BCR–ABL1, and then subsequently ...

CAS 80418-25-3 20(S)-Notoginsenoside R2

20(S)-Notoginsenoside R2
(CAS: 80418-25-3)

20(S)-Notoginsenoside R2 is a natural product extracted from the roots of Panax notoginseng (Burk.) F.H.Chen. It has neuroprotection against 6-OHDA-induced neur...

CP-690550A
(CAS: 1243290-37-0)

This active molecular is a novel Janus Kinase 3 (JAK3) inhibitor. CP-690550A is an immunosuppressant for the treatment of rheumatoid arthritis, psoriasis, trans...

CAS 273727-89-2 ZM 39923

ZM 39923
(CAS: 273727-89-2)

ZM 39923 inhibits Janus kinase (IC50=10 nM).

CAS 1271022-90-2 BMS-911543

BMS-911543
(CAS: 1271022-90-2)

BMS-911543 is an orally available small molecule targeting a subset of Janus-associated kinase (JAK) with potential antineoplastic activity. JAK2 inhibitor BMS-...

AC410
(CAS: 1361415-84-0)

AC410 is a Janus kinase 2 (JAK2) inhibitor with Kd of 0.18 nM. AC410 is selective for JAK2 and Kd is 2.5 nM for JAK1 and 5nM for JAK3. Phase I for the treatment...

Chemical Structure

CAS 1092578-48-7 (3S,4R)-Tofacitinib

Quick Inquiry

Verification code

Featured Items