(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile sulfate
![(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile sulfate Structure](CAS2/GIF/1092939-16-6.gif)
- CAS No.
- 1092939-16-6
- Chemical Name:
- (betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile sulfate
- Synonyms
- INCB018424 (sulfate);Ruxolitinib (sulfate);Ruxolitinib sulfate (INC 424, INCB 18424, INCB 018424, Jakafi, Jakavi);(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile sulfate;BETA-CYCLOPENTYL-4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-(BETAR)-1H-PYRAZOLE-1-PROPANENITRILE, SULFATE
- CBNumber:
- CB02509992
- Molecular Formula:
- C17H20N6O4S
- Molecular Weight:
- 404.45
- MDL Number:
- MOL File:
- 1092939-16-6.mol
- MSDS File:
- SDS
(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile sulfate price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Crysdot | CD31004607 | Ruxolitinibsulfate 98+% | 1092939-16-6 | 5mg | $56 | 2021-12-16 | Buy |
| Crysdot | CD31004607 | Ruxolitinibsulfate 98+% | 1092939-16-6 | 10mg | $90 | 2021-12-16 | Buy |
| Crysdot | CD31004607 | Ruxolitinibsulfate 98+% | 1092939-16-6 | 50mg | $207 | 2021-12-16 | Buy |
| Chemenu | CM152415 | (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrilesulfate 98% | 1092939-16-6 | 100mg | $347 | 2021-12-16 | Buy |
| Crysdot | CD31004607 | Ruxolitinibsulfate 98+% | 1092939-16-6 | 100mg | $371 | 2021-12-16 | Buy |
(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile sulfate Chemical Properties,Uses,Production
Description
Ruxolitinib sulfate is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
in vitro
In Vitro:Ruxolitinib sulfate is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib potently and selectively inhibits JAK2V617F-mediated signaling and proliferation, markedly increases apoptosis in a dose dependent manner, and at 64 nM results in a doubling of cells with depolarized mitochondria in Ba/F3 cells. Ruxolitinib demonstrates remarkable potency against erythroid colony formation with IC50 of 67 nM, and inhibits proliferating of erythroid progenitors from normal donors and polycythemia vera patients with IC50 values of 407 nM and 223 nM, respectively[1].
in vivo
In Vivo:Ruxolitinib (180 mg/kg, orally, twice a day) results in survive rate of greater than 90% by day 22 and markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminated neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects in a JAK2V617F-driven mouse model[1]. In the Ruxolitinib group, the primary end point is reached in 41.9% of patients, as compared with 0.7% in the placebo group in the double-blind trial of myelofibrosis. Ruxolitinib results in maintaining of reduction in spleen volume and improvement of 50% or more in the total symptom score[2]. Ruxolitinib (15 mg twice daily) treatment leads a total of 28% of the patients to have at least a 35% reduction in spleen volume at week 48 in patients with myelofibrosis, as compared with 0% in the group receiving the best available therapy. The mean palpable spleen length has decreased by 56% with Ruxolitinib but has increased by 4% with the best available therapy at week 48. Patients in the ruxolitinib group has an improvement in overall quality-of-life measures and a reduction in symptoms associated with myelofibrosis[3].
References
References:[1]. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117. [2]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807. [3]. Harrison C, et al. JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis. N Engl J Med. 2012 Mar 1;366(9):787-98.
(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile sulfate Preparation Products And Raw materials
Raw materials
Preparation Products
(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile sulfate Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49391 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
| MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4863 | 58 |
| LETOPHARM LIMITED | +86-21-5821 5861 | sales@letopharm.com | China | 2384 | 58 |
| SPIRO PHARMA | eric_feng1954@126.com | China | 9254 | 55 | |
| BOC Sciences | 16314854226 | info@bocsci.com | United States | 9926 | 65 |
| Amatek Scientific Co. Ltd. | 0512-56316828 | info@amateksci.com | China | 28821 | 58 |
| Musechem | +1-800-259-7612 | info@musechem.com | United States | 4662 | 60 |
| Supplier | Advantage |
|---|---|
| CONIER CHEM AND PHARMA LIMITED | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 58 |
| InvivoChem | 58 |
| Amadis Chemical Company Limited | 58 |
| MedChemexpress LLC | 58 |
| LETOPHARM LIMITED | 58 |
| SPIRO PHARMA | 55 |
| BOC Sciences | 65 |
| Amatek Scientific Co. Ltd. | 58 |
| Musechem | 60 |