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
- Molecular Weight:
- 285.34
- MDL Number:
- MFCD31697544
- MOL File:
- 1792180-81-4.mol
1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one Properties
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) |
pka | 13.03±0.50(Predicted) |
form | powder |
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 |
FDA UNII | 2OYE00PC25 |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H302-H315-H319-H335 |
Precautionary statements | P261-P305+P351+P338 |
1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one price More Price(11)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | PZ0316 | PF-06651600 ≥98% (HPLC) | 1792180-81-4 | 5MG | $105 | 2023-06-20 | Buy |
Sigma-Aldrich | PZ0316 | PF-06651600 ≥98% (HPLC) | 1792180-81-4 | 25MG | $339 | 2023-06-20 | Buy |
Usbiological | 462323 | PF-06651600 | 1792180-81-4 | 1mg | $319 | 2021-12-16 | Buy |
Usbiological | 474159 | PF06651600 | 1792180-81-4 | 100mg | $2315 | 2021-12-16 | Buy |
ChemScene | CS-0020243 | Ritlecitinib 99.98% | 1792180-81-4 | 5mg | $80 | 2021-12-16 | Buy |
1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one Chemical Properties,Uses,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
1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Jinan Million Pharmaceutical Co., Ltd | 0531-68659554 +8613031714605 | info@millionpharm.com | China | 252 | 58 |
Jinan Jianfeng Chemical Co., Ltd | 0531-88110457; +8615562555968 | info@pharmachemm.com | China | 248 | 58 |
Hebei Mojin Biotechnology Co., Ltd | +86 13288715578 +8613288715578 | sales@hbmojin.com | China | 12840 | 58 |
Wuhan senwayer century chemical Co.,Ltd | +undefined-27-86652399 +undefined13627115097 | market02@senwayer.com | China | 902 | 58 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32957 | 60 |
Jinan Carbotang Biotech Co.,Ltd. | +8615866703830 | figo.gao@foxmail.com | China | 8497 | 58 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32165 | 58 |
NINGBOBENKANGJS PHARMTECHCO., LTD | +8615990591583 15990591583 | CHINA | 2029 | 58 | |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
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
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2024-11-25 | Ritlecitinib
1792180-81-4
|
US $50.00 / g | 10g | 99% | 10KG/M | Jinan Million Pharmaceutical Co., Ltd | ||
2024-11-25 | Ritlecitinib
1792180-81-4
|
US $0.00-0.00 / kg | 0.10000000149011612kg | 99% | 5000kg | Jinan Jianfeng Chemical Co., Ltd | ||
2024-11-17 | Ritlecitinib
1792180-81-4
|
US $39.00-113.00 / mg | 99.92% | 10g | TargetMol Chemicals Inc. |
- Ritlecitinib
1792180-81-4
- US $50.00 / g
- 99%
- Jinan Million Pharmaceutical Co., Ltd
- Ritlecitinib
1792180-81-4
- US $0.00-0.00 / kg
- 99%
- Jinan Jianfeng Chemical Co., Ltd
- Ritlecitinib
1792180-81-4
- US $39.00-113.00 / mg
- 99.92%
- TargetMol Chemicals Inc.
1792180-81-4(1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one)Related Search:
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