(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile
Ruxolitinib
CAS: 941678-49-5;1092939-17-7
Molecular Formula: C17H18N6
(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile - Names and Identifiers
(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile - Physico-chemical Properties
| Molecular Formula | C17H18N6 |
| Molar Mass | 306.37 |
| Density | 1.40 |
| Melting Point | 84-89°C |
| Solubility | Soluble in DMSO (up to 28 mg/ml) or in Ethanol (up to 15 mg/ml with warming). |
| Appearance | White powder. |
| Color | White |
| pKa | 11.63±0.50(Predicted) |
| Storage Condition | -20° |
| 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. |
(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile - Risk and Safety
| HS Code | 29335990 |
(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.473 ml | 12.365 ml | 24.73 ml |
| 5 mM | 0.495 ml | 2.473 ml | 4.946 ml |
| 10 mM | 0.247 ml | 1.237 ml | 2.473 ml |
| 5 mM | 0.049 ml | 0.247 ml | 0.495 ml |
Last Update：2024-01-02 23:10:35
(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile - Reference Information
| pharmacological action | myelofibrosis (MF) is a rare disease of bone marrow hyperplasia, bone marrow is replaced by scar tissue in the body, resulting in the production of blood cells in organs such as the liver and spleen, characterized by splenomegaly, anemia, leukopenia and thrombocytopenia, and varying degrees of bone sclerosis. Symptoms include Fatigue, abdominal discomfort, pain under the ribs, muscle and bone pain, itching and night sweats. ruxolitinib is the first FDA-approved oral drug for the treatment of myelofibrosis. It is a tyrosine kinase inhibitor, a small molecule inhibitor of protein kinases JAK1 and JAK2, and is indicated for the treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis, and post-essential thrombocythemia myelofibrosis. on 29 August 2012, the first drug approved in the European Union for the treatment of myelofibrosis-ruxolitinib, and ruxolitinib for the treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, myelofibrosis after polycythemia vera and myelofibrosis after essential thrombocythemia. At present, Ruxolitinib has been approved by more than 50 countries, including the European Union, Canada and some Asian, Latin American and South American countries. Novartis Pharmaceuticals has authorized the development and commercialization rights of Ruxolitinib outside the United States from Incyte. Both the European Commission and the FDA have granted Ruxolitinib orphan status for the treatment of myelofibrosis. Currently, Incyte has been marketed under the trade name Jakafi in the United States for the treatment of intermediate or high-risk myelofibrosis. Figure 1 shows |
| Application status | Ruxolitinib (also known as ruxotinib) is a kinase inhibitor, for the treatment of intermediate or high-risk myelofibrosis, including patients with primary myelofibrosis, myelofibrosis after polycythemia vera and myelofibrosis after essential thrombocythemia. ruxolitinib (Jakavi), an oral JAK1 and JAK2 tyrosine kinase inhibitor, was approved in the European Union in August 2012 for the treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, myelofibrosis after polycythemia vera and myelofibrosis after essential thrombocythemia. currently, rusolitinib Jakavi has been approved in more than 50 countries worldwide, including the European Union, Canada and some Asian, Latin American and South American countries. Novartis authorized the development and commercialization rights of Ruxolitinib outside the United States from Incyte. Both the European Commission and the FDA have granted Ruxolitinib orphan status for the treatment of myelofibrosis. Currently, Incyte has been marketed under the trade name Jakafi in the United States for the treatment of intermediate or high-risk myelofibrosis. |
| biological activity | ruxolitinib (INCB18424) is potent, selective JAK1 and JAK2 inhibitors (IC50 2.7 and 4.5nM, respectively) have potent anti-tumor and immunomodulatory activities. Ruxolitinib inhibited IL-6 signal (IC50 = 281nM) and JAK2V617F Ba/F3 cell proliferation (IC50 = 127nM). Ruxolitinib also inhibited STAT3 phosphorylation in wild-type JAK2 and JAK2 V617F mutant patients. Clinical application it can significantly reduce the level of circulating inflammatory cytokines related. ruxolitinib has a potent effect in rat adjuvant arthritis and multiple Murine Arthritis models. |
| indications | ruxolitinib is a kinase inhibitor indicated for the treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, myelofibrosis after polycythemia vera and myelofibrosis after essential thrombocythemia. |
| dosage | (1) for patients with platelet count greater than 200/μL, ruxolitinib the starting dose was 20mg orally administered twice daily, while patients had a platelet count of 15mg twice daily between 100/μL and 200/μL. (2) complete blood count was performed prior to initiation of treatment with ruxolitinib. Complete blood counts were monitored every 2 to 4 weeks, and the dose was adjusted for platelet count reduction. (3) increase the dose according to response and due to recommendation to a maximum of 25mg twice daily. If no decrease in the spleen or no improvement in symptoms 6 months after termination. |
| adverse reactions | The most common hematologic adverse reactions (incidence> 20%) were platelet count decreased and anemia. The most common non-hematologic adverse events (incidence> 10%) were ecchymosis, vertigo, and Head Pain. |
| other clinical studies | Columbia University Medical Center A study was conducted to test whether an approved drug for treating bone marrow disease could help people get rid of alopecia areata. The study found that seven women and five men who took part in human testing, after taking one of the drugs, Ruxolitinib, most people have a great improvement in their condition. Some of their findings were published in the journal Nature Medicine. |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 02:00:12
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View History
(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile
L-4-羟脯氨酸叔丁酯
3-丁烯溴化镁,0.5 M IN THF
P-METHOXYBENZYL CHLORIDE
Trisodium (5-((4,5-dihydro-3-methyl-5-oxo-1-phenyl-1H-pyrazol-4-yl)azo)-4-hydroxy-3-((2-hydroxy-3-nitro-5-sulphophenyl)azo)naphthalene-2,7-disulphonato(5-))nickelate(3-)
2-(6-(三氟甲基)咪唑并[1,5-a]吡啶-3-基)乙酸
2-(4-(Trifluoromethyl)pyridin-2-yl)acetate (sodium)
2-[2-(anilino-phenyl-methylidene)azaniumylphenoxy]ethyl-dipropan-2-yl- azanium dichloride
cis-Diammine(pyridine)chloroplatinum(II) chloride
Z-PROLINE-OSU
L-4-羟脯氨酸叔丁酯
3-丁烯溴化镁,0.5 M IN THF
P-METHOXYBENZYL CHLORIDE
Trisodium (5-((4,5-dihydro-3-methyl-5-oxo-1-phenyl-1H-pyrazol-4-yl)azo)-4-hydroxy-3-((2-hydroxy-3-nitro-5-sulphophenyl)azo)naphthalene-2,7-disulphonato(5-))nickelate(3-)
2-(6-(三氟甲基)咪唑并[1,5-a]吡啶-3-基)乙酸
2-(4-(Trifluoromethyl)pyridin-2-yl)acetate (sodium)
2-[2-(anilino-phenyl-methylidene)azaniumylphenoxy]ethyl-dipropan-2-yl- azanium dichloride
cis-Diammine(pyridine)chloroplatinum(II) chloride
Z-PROLINE-OSU