性能参数

产品名称

Ruxolitinib (INCB018424)

规格

10mM (in 1mL DMSO) 5mg 25mg 100mg

货号

GOY-Y3753

 含量

>98.00%

CAS

941678-49-5

别名

Ruxolitinib,INCB018424,INCB-018424

化学名

(3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile

分子式

C17H18N6

分子量

分子量 306.37

溶解度

≥ 15.32mg/mL in DMSO

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

Ruxolitinib (INCB18424) is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over 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].

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].

  7112-39-2  (6-氨基吡啶-2-基)乙酸乙酯  71469-82-4

N-BOC-乙烯胺  7150-72-3  异氰酸叔丁酯  7188-38-7

2，4-二甲基噻唑-5-羧酸乙酯  7210-77-7  2,6-二氯苯磺酰氯  6579-54-0

氨噻肟酸  65872-41-5  5-氨基颉草酸  660-88-8

正己醛  66-25-1  2-氯-4-甲基苯酚  6640-27-3

氘代丙酮  666-52-4  噻奈普汀  66981-73-5

UNC 064210mM (in 1mL DMSO) 10mg 50mg>98.00%Cas No. 1481677-78-4C29H44F2N6O2

UF 01010mM (in 1mL DMSO) 10mg 50mg>98.00%Cas No. 537672-41-6C11H15BrN2O

Tyk2-IN-8100mg 250mg 500mg>98.00%Cas No. 2127109-84-4C20H17N9

Tyk2-IN-7100mg 250mg 500mg>98.00%Cas No. 1609391-90-3C18H15D3N6O3S

Valproic acid sodium salt (Sodium valproate)10mM (in 1mL DMSO) 5g 10g>98.00%Cas No. 1069-66-5C8H15NaO2

Valproic acid10mM (in 1mL DMSO) 5g 10g>98.00%Cas No. 99-66-1C8H16O2

Valemetostat tosylate100mg 250mg 500mg>98.00%Cas No. 1809336-93-3C33H42ClN3O7S