Ruxolitinib
- CAS No.
- 941678-49-5
- Chemical Name:
- Ruxolitinib
- Synonyms
- Jakafi;Roxolitinib;(R)-3-(4-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile;(R)-Ruxolitinib;CS-163;Pridazole;Rusotinib;Russolinib;Benzalolin;Ruxolitinib
- CBNumber:
- CB02499581
- Molecular Formula:
- C17H18N6
- Molecular Weight:
- 306.37
- MOL File:
- 941678-49-5.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/5/29 17:03:55
| Melting point | 84-89°C |
|---|---|
| Density | 1.40 |
| storage temp. | -20° |
| solubility | Soluble in DMSO (up to 28 mg/ml) or in Ethanol (up to 15 mg/ml with warming). |
| form | White powder. |
| pka | 11.63±0.50(Predicted) |
| color | White |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| InChI | InChI=1/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/s3 |
| InChIKey | HFNKQEVNSGCOJV-UJHUVDBMNA-N |
| SMILES | [C@@H](C1CCCC1)(N1N=CC(C2N=CN=C3NC=CC=23)=C1)CC#N |&1:0,r| |
| CAS DataBase Reference | 941678-49-5 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS07,GHS08 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H302-H360FD | |||||||||
| Precautionary statements | P202-P280 | |||||||||
| HS Code | 29335990 | |||||||||
| NFPA 704 |
|
Ruxolitinib Chemical Properties,Uses,Production
Description
In November 2011, the U.S. FDA approved ruxolitinib (INCB018424) for the treatment of patients with intermediate or high-risk myelofibrosis. Ruxolitinib is an ATP-competitive inhibitor of JAK1 and JAK2 (IC50's of 3.3±1.2 nM and 2.8±1.2 nM, respectively) and inhibition occurs regardless of the JAK2V617F mutational status. Ruxolitinib is a moderately potent inhibitor of the related JAK, TYK2 (IC50=19±3.2 nM) but is selective versus JAK3 (IC50=428±243 nM). It was also selective versus a panel of 26 other kinases at concentrations approximately 100-fold the IC50 of JAK1 and JAK2. Inhibition of JAK1 and JAK2 downregulates the JAK-signal transducer and activator of transcription (STAT) pathway, inhibiting myeloproliferation, inducing apoptosis, and reducing numerous cytokine plasma levels.
Characteristics
Class: non-receptor tyrosine kinase
Treatment: MF, PV, cGVHD
Oral bioavailability >95%
Elimination half-life = 3 h
Protein binding = 97%
Uses
Ruxolitinib is a selective Janus tyrosine kinase (JAK1 and JAK2) inhibitor used in the treatment of myeloproliferative neoplasms and psoriasis.
Indications
The JAK family includes four isoforms, JAK1, JAK2, JAK3, and tyrosine kinase (TYK2). Ruxolitinib (Jakafi(R), Incyte Corp.) was the first approved JAK inhibitor, which inhibits both JAK1 and JAK2, used for the treatment of different types of myelofibrosis. Tofacitinib (Xeljanz(R), Pfizer) was approved by FDA as a JAK3-selective inhibitor for the treatment of rheumatoid arthritis and is one of the only two FDA-approved kinase inhibitors for non-oncological indications.
Definition
ChEBI: A pyrazole substituted at position 1 by a 2-cyano-1-cyclopentylethyl group and at position 3 by a pyrrolo[2,3-d]pyrimidin-4-yl group. Used as the phosphate salt for the treatment of patients with intermediate or high-risk myelofibrosis, includ ng primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis.
Ruxolitinib Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| CHEMSWORTH | +91-261-2397244 | New Delhi, India | 6707 | 30 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| Zhengzhou Anhuida Chemical Co., Ltd | +8615903659408 | China | 294 | 58 | Inquiry |
| TAIZHOU YUXIN BIOTECHNOLOGY CO,.LTD | +86-576-88902229;+86-0576-88902229 +8613968687450 | China | 158 | 58 | Inquiry |
| Hebei Mojin Biotechnology Co., Ltd | +86 13288715578 +8613288715578 | China | 12460 | 58 | Inquiry |
| Senova Technology Co. Ltd. | +86-0755-86703119 +8618503098836 | China | 350 | 58 | Inquiry |
| Hebei Duling International Trade Co. LTD | +8617333973358 | China | 15440 | 58 | Inquiry |
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