ChemicalBook > CAS DataBase List > Baricitinib phosphate salt

Baricitinib phosphate salt

IC50 & Target In Vivo

Product Name: Baricitinib phosphate salt
CAS No.: 1187595-84-1
Chemical Name: Baricitinib phosphate salt
Synonyms: INCB-28050;INCB424-ANALOGUE;LY-3009104 phosphate;INCB028050 phosphate);INCB-28050; LY3009104;Baricitinib (phosphate);Baricitinib phosphate salt;INCB424-Analogue (INCB-28050);Baricitinib phosphate, 10 mM in DMSO;Baricitinib phosphate (LY3009104 phosphate
CBNumber: CB72621127
Molecular Formula: C16H20N7O6PS
Formula Weight: 469.412061
MOL File: 1187595-84-1.mol

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Baricitinib phosphate salt Property

storage temp.: Store at -20°C
solubility: insoluble in EtOH; insoluble in H2O; ≥172.6 mg/mL in DMSO
form: White powder.
color: White to yellow
InChIKey: FBPOWTFFUBBKBB-UHFFFAOYSA-N
SMILES: C(#N)CC1(N2C=C(C3=NC=NC4NC=CC=43)C=N2)CN(S(CC)(=O)=O)C1.P(O)(O)(O)=O

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TRC

Product number: B118693
Product name: BaricitinibPhosphate
Packaging: 5mg
Price: $45
Updated: 2021/12/16

TRC

Product number: B118693
Product name: BaricitinibPhosphate
Packaging: 50mg
Price: $205
Updated: 2021/12/16

ApexBio Technology

Product number: A3222
Product name: Baricitinibphosphate
Packaging: 50mg
Price: $210
Updated: 2021/12/16

AK Scientific

Product number: SYN1117
Product name: Baricitinibphosphate
Packaging: 5mg
Price: $295
Updated: 2021/12/16

Adipogen Life Sciences

Product number: SYN-1117-M010
Product name: Baricitinibphosphatesalt
Purity: ≥95%
Packaging: 10mg
Price: $416
Updated: 2021/12/16

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Baricitinib phosphate salt Chemical Properties,Usage,Production

IC50 & Target

JAK2: 5.7 nM (IC50) JAK1: 5.9 nM (IC50) Tyk2: 53 nM (IC50) JAK3: 560 nM (IC50)

In Vivo

Baricitinib phosphate treatment, compares with vehicle, inhibits the increase in hind paw volumes during the 2 wk of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 or 10 mg/kg. Because baseline paw volume measurements are taken on treatment day 0-in animals with significant signs of disease-it is possible to have >100% inhibition in animals showing marked improvement in swelling[1]. Baricitinib (0.7 mg/day) treated mice exhibits substantially reduced inflammation as assessed by H&E staining, reduced CD8 infiltration, and reduced MHC class I and class II expression when compared with vehicle-control treated mice. CD8+NKG2D+ cells, critical effectors of disease in murine and human alopecia areata (AA), are greatly diminished in Baricitinib treated mice compare with vehicle control treated mice.

Uses

Baricitinib phosphate salt is a JAK1 and JAK2 inhibitor and have been used as a promising treatment for rheumatoid arthritis.

Biological Activity

Baricitinib phosphate salt is a direct and indirect inhibition of the jaks has demonstrated rapid and sustained improvement in clinical measures of disease. baricitinib phosphate (incb 028050) is a selective jak1 and jak2 inhibitor.

Synthesis

1187594-09-7

1187595-84-1

General procedure for the synthesis of [1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl]acetonitrile phosphates from baricitinib: Barectinib (0.30 g, 0.8 mmol) was dissolved in boiling acetonitrile (7 ml), followed by the titrative addition, over a 30-minute period, of phosphoric acid ( 0.20 g, 2.1 equivalents, 85% aqueous solution) solution in methanol (1.2 ml). The reaction mixture was stirred at 68 °C for 1 h, then slowly cooled to room temperature and continued stirring overnight. The precipitate was collected by filtration and dried at 35 °C for 18 h at 200 mbar to give baricitinib phosphate of form C as a white powder (376 mg, 99.2% yield). The stoichiometric ratio was 1:1.14.

in vitro

In cell-based assays, Baricitinib phosphate proves to be a potent inhibitor of JAK signaling and function. In PBMCs, Baricitinib inhibits IL-6-stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively. In isolated naive T-cells, INCB028050 also inhibits pSTAT3 stimulated by IL-23 (IC50=20 nM). Importantly, this inhibition prevented the production of two pathogenic cytokines (IL-17 and IL-22) produced by Th17 cells-a subtype of helper T cells with demonstrable inflammatory and pathogenic properties-with an IC50 value of 50 nM. In stark contrast, the structurally similar but ineffective JAK1/2 inhibitors INCB027753 and INCB029843 has no significant effect in any of these assays systems when tested at concentrations up to 10 μM.

in vivo

significant efficacy was achieved in the rat adjuvant arthritis model with doses of baricitinib phosphate providing partial and/or periodic inhibition of jak1/jak2 and no inhibition of jak3. baricitinib phosphate was also effective in multiple murine models of arthritis, with no evidence of suppression of humoral immunity or adverse hematologic effects [2].

IC 50

JAK2: 5.7 nM (IC₅₀); JAK1: 5.9 nM (IC₅₀); Tyk2: 53 nM (IC₅₀); JAK3: 560 nM (IC₅₀)

References

[1] fridman js, scherle pa, collins r, burn tc, li y, li j, covington mb, thomas b, collier p, favata mf, wen x, shi j, mcgee r, haley pj, shepard s, rodgers jd, yeleswaram s, hollis g, newton rc, metcalf b, friedman sm, vaddi k. selective inhibition of jak1 and jak2 is efficacious in rodent models of arthritis: preclinical characterization of incb028050. j immunol. 2010;184(9):5298-307.

Baricitinib phosphate salt Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Baricitinib phosphate salt manufacturers

Shaanxi Xianhe Biotech Co., Ltd

Product: Baricitinib phosphate 1187595-84-1
Price: US $0.00/kg
Min. Order: 1kg
Purity: 0.99
Supply Ability: 1000kg
Release date: 2025-04-18

henan kanbei chemical co.,ltd

Product: Baricitinib phosphate salt 1187595-84-1
Price: US $0.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 1000kg
Release date: 2022-09-26

Zhuozhou Wenxi import and Export Co., Ltd

Product: Baricitinib phosphate salt 1187595-84-1
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-06-27

1187595-84-1, Baricitinib phosphate saltRelated Search:

Bromothymol Blue Butyl stearate 1146629-80-2 Ruxolitinib phosphate

2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile phosphate

Baricitinib phosphate salt

INCB-28050

INCB-28050; LY3009104

Baricitinib (phosphate)

[1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl]acetonitrile phosphate

INCB424-Analogue (INCB-28050)

INCB-028050;LY-3009104;INCB 028050;LY 3009104;INCB028050;LY3009104

Baricitinib phosphate (LY3009104 phosphate

BARICITINIB PHOSPHATE (LY3009104 PHOSPHATE; INCB028050 PHOSPHATE)

INCB028050 phosphate)

LY-3009104 phosphate

Baricitinib phosphate (LY-3009104, INCB-028050, Olumiant)

Baricitinib phosphate, 10 mM in DMSO

INCB424-ANALOGUE

2-(3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile, phosphate salt

1187595-84-1

C16H17N7O2SH3PO4

C16H20N7O6PS

C16H17N7O2SH3O4P

Inhibitors