1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one

Product Name: 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one
CAS No.: 1792180-81-4
Chemical Name: 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one
Synonyms: Ritlecitinib;PF-06651600;CS-2733;EOS-61890;Ritlecitinib (PF-06651600);PF-06651600;PF 06651600;PF06651600;Ritlecitinib free base PF-06651600;Janus kinase,Inhibitor,inhibit,PF06651600,Ritlecitinib,JAK,PF 06651600;1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2;1-[(2S,5R)-2-Methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one
CBNumber: CB23142473
Molecular Formula: C15H19N5O
Formula Weight: 285.34
MOL File: 1792180-81-4.mol

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1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one Property

Density: 1.272±0.06 g/cm3(Predicted)
storage temp.: room temp
solubility: DMSO:100.0(Max Conc. mg/mL);350.4(Max Conc. mM)
H2O:5.0(Max Conc. mg/mL);17.5(Max Conc. mM)
form: powder
pka: 13.03±0.50(Predicted)
color: white to beige
InChI: InChI=1S/C15H19N5O/c1-3-13(21)20-8-11(5-4-10(20)2)19-15-12-6-7-16-14(12)17-9-18-15/h3,6-7,9-11H,1,4-5,8H2,2H3,(H2,16,17,18,19)/t10-,11+/m0/s1
InChIKey: CBRJPFGIXUFMTM-WDEREUQCSA-N
SMILES: C(N1C[C@H](NC2N=CN=C3NC=CC3=2)CC[C@@H]1C)(=O)C=C

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

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

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

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: PZ0316
Product name: PF-06651600
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $105
Updated: 2023/06/20

Sigma-Aldrich

Product number: PZ0316
Product name: PF-06651600
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $339
Updated: 2023/06/20

Usbiological

Product number: 462323
Product name: PF-06651600
Packaging: 1mg
Price: $319
Updated: 2021/12/16

Usbiological

Product number: 474159
Product name: PF06651600
Packaging: 100mg
Price: $2315
Updated: 2021/12/16

ChemScene

Product number: CS-0020243
Product name: Ritlecitinib
Purity: 99.98%
Packaging: 5mg
Price: $80
Updated: 2021/12/16

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1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one Chemical Properties,Usage,Production

Description

Ritlecitinib, a dual JAK3/TEC inhibitor, was granted FDA breakthrough status for treating alopecia areata (autoimmune-induced hair loss) in September 2018. Promising phase 3 trial results in alopecia areata were reported by Pfizer in August 2021, placing it in competition with Lilly/Incyte’s Olumiant. It is also used in clinical studies to treat vitiligo, rheumatoid arthritis, Crohn’s disease, and ulcerative colitis. Ritlecitinib achieved high JAK3 selectivity via covalent interaction with a unique cysteine residue (Cys909) in the catalytic domain.

Characteristics

Primary targets: JAK3/TEC
Class: non-receptor tyrosine kinase
Treatment: alopecia areata (phase III)
Protein binding = 14%

Biochem/physiol Actions

PF-06651600 is a potent and selective JAK3 inhibitor.

Pharmacokinetics

Ritlecitinib exhibited low clearance in rats and dogs, contributing to its good oral bioavailability (85% in rats and 109% in dogs). Its lower oral bioavailability in monkeys (56%) primarily resulted from its fast clearance. The pharmacokinetic properties are directly linked to its stability in hepatocytes and whole blood, demonstrating the power of in vitro assays to predict in vivo pharmacokinetic parameters. The good oral bioavailability obtained from rats and dogs was a combination of high passive permeability, high aqueous solubility (>2 mg/mL), and low hepatic clearance. Ritlecitinib underwent CYP3A4-mediated oxidation of the acrylamide and piperidine ring and glutathione conjugated with the acrylamide. Allometric scaling predicted an oral bioavailability of 90% and a half-life of 2 h in humans, which need to be verified in clinical trials.

1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one Preparation Products And Raw materials

Raw materials

Preparation Products

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1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one Suppliers

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TargetMol Chemicals Inc.

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View Lastest Price from 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one manufacturers

Jinan Million Pharmaceutical Co., Ltd

Product: Ritlecitinib 1792180-81-4
Price: US $50.00/g
Min. Order: 10g
Purity: 99%
Supply Ability: 10KG/M
Release date: 2023-08-17

Jinan Jianfeng Chemical Co., Ltd

Product: Ritlecitinib 1792180-81-4
Price: US $0.00-0.00/kg
Min. Order: 0.10000000149011612kg
Purity: 99%
Supply Ability: 5000kg
Release date: 2024-08-07

Wuhan Senwayer Century Chemical Co.,Ltd

Product: Ritlecitinib 1792180-81-4
Price: US $0.00/g
Min. Order: 1g
Purity: 99% min
Supply Ability: 20 kg
Release date: 2024-08-20

1792180-81-4, 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-oneRelated Search:

PF-06700841 tosylate PF-06650833 PF-06447475 Lorlatinib (PF-06463922) 3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide 2-[[(2E)-3-(2-NAPHTHALENYL)-1-OXO-2-BUTEN-1-YL]AMINO]BENZOIC ACID Upadacitinib Q-VD-OPh hydrate N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide H3B-6527 Senexin B 2-(2-((4-bromophenyl)amino)-2-oxoethoxy)-N-(2-(methyl(phenyl)amino)-2-oxoethyl)benzamide (S)-4-(4-((2-(3,5-diMethylphenyl)pyrrolidin-1-yl)Methyl)phenoxy)-3-fluorobenzaMide BMS-986205 Budiodarone tartrate COH-29

PF-06651600

EOS-61890

1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one

1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2

CS-2733

PF-06651600;PF 06651600;PF06651600

1-[(2S,5R)-2-methyl-5(7H-pyrrolo[2,3-d]pyrimidine-4-ylamino)-1-piperidinly]-2-propen-1-one malonate,PF06651600

Ritlecitinib

2-Propen-1-one, 1-[(2S,5R)-2-methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-

1-[(2S,5R)-2-Methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one

Ritlecitinib (PF-06651600)

Janus kinase,Inhibitor,inhibit,PF06651600,Ritlecitinib,JAK,PF 06651600

1-[(2S,5R)-5-[[7H-Pyrrolo[2,3-d]-4-pyrimidinyl]amino]-2-methyl-1-piperidyl]-2-propen-1-one

Ritlecitinib free base PF-06651600

1792180-81-4

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