Ruxolitinib (INCB018424)

目录号:S1378

Ruxolitinib (INCB018424) Chemical Structure

Molecular Weight(MW): 306.37

Ruxolitinib (INCB018424)是第一个应用于临床的,有效的,选择性JAK1/2抑制剂,在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1, JAK2与作用于JAK3相比,选择性高130多倍。

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RMB 1703.45 现货
RMB 1317.79 现货
RMB 1896.85 现货
RMB 2633.61 现货
RMB 6542.21 现货
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客户购买Selleck的此次产品后发表的文献36篇:

客户使用该产品的6个实验数据:

  • a, Phospho- and total STAT1 in MDA-MB-453 cells treated with abemaciclib with or without ruxolitinib for 7 days.

    Nature, 2017, 548(7668):471-475. Ruxolitinib (INCB018424) purchased from Selleck.

    STAT3 phosphorylation as determined by phospho flow, mixed lymphocyte reactions containing BALB/c spleen-derived CD4+ T cells co-cultured with or without C57BL/6 BM-derived DC preactivated with 20 ng/mL LPS.

    Blood 2014 123(24), 3832-42. Ruxolitinib (INCB018424) purchased from Selleck.

  • BMDMs were isolated from wild-type mice and incubated in the different concentrations of Ruxolitinib for 1 h before stimulation with 500 U/ml IFN-β for 30 min. Levels of GAPDH as well as total and phospho-Tyr705 STAT3 were determined by immunoblotting.

    J Immunol 2012 189(6), 2784-92. Ruxolitinib (INCB018424) purchased from Selleck.

    Miniscule 10 PFU amount of VA7-EGFP results in productive infection only in CT26LacZ cells whereas the self-limiting infection can be rescued with JAK/STAT inhibitor Ruxolitinib in CT26WT cells counteracting also the effects of exogenous IFNβ (100 U/ml) pre-treatment. Scale bar: 200 um.

    Gene Ther 2014 10.1038/gt.2014.83. Ruxolitinib (INCB018424) purchased from Selleck.

  • INCB018424 administration reverses the protective effects of ALA on ONC retinas. A-C: Representative micrographs (200× magnification) of retinal whole mounts obtained from three groups stained with anti-RNA-binding protein with multiple splicing (Rbpms) antibody (green). Sampling location: 2 mm temporal to the optic disc. Sampling field size: 439 × 330 μm2 (20× objective lens). Scale bar: 50 μm. D: Quantitative analysis of Rbpms-positive cells under different experimental conditions (mean ± standard error of the mean [SEM], n = 6 per group). The average number of Rbpms-positive cells/mm2 was calculated. ONC = optic nerve crush animal; ALA-ONC = alpha lipoic acid (ALA) animal pretreated 1 day before ONC; ALA-ONC+I = ALA animal pretreated 1 day before ONC, followed by INCB018424. *** p<0.001, ** p<0.01 compared to the ONC group, ### p<0.001 compared to the ALA-ONC group at the same time point

    Mol Vis, 2016, 22:1122-1136. Ruxolitinib (INCB018424) purchased from Selleck.

     

    HS578T cells were treated with indicated amount of inhibitor for 18 hr. The cells were lysed by cell lysis buffer (20 mM Tris-Cl (pH 8.0); 0.5 M NaCl; 0.25% Triton X-100; 1 mM EDTA; 1 mM EGTA; 10 mM β-glycerophosphate; 10 mM NaF; 300 µM Na3VO4; 1 mM benzamidine) containing 1 mM DTT and 2 µM PMSF. Western blot analyses were performed using cleared cell lysates resolved on sodium dodecyl sulfate (SDS)-polyacrylamide gels, transferred onto polyvinylidene difluoride (PVDF) membranes (Millipore, Billerica, MA), and probed with specific antibodies using standard procedures. Chemiluminescence reagent was purchased from  Thermo Scientific (Rockford, IL). Horseradish peroxidase-conjugated secondary antibodies from Sigma (St. Louis, MO).

    Yong Weon Yi Georgetown University. Ruxolitinib (INCB018424) purchased from Selleck.

产品安全说明书

JAK抑制剂选择性比较

生物活性

产品描述 Ruxolitinib (INCB018424)是第一个应用于临床的,有效的,选择性JAK1/2抑制剂,在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1, JAK2与作用于JAK3相比,选择性高130多倍。
靶点
JAK2 [1]
(Cell-free assay)
JAK1 [1]
(Cell-free assay)
2.8 nM 3.3 nM
体外研究

在Ba/F3细胞和HEL细胞中,INCB018424有效地和有选择性地抑制JAK2V617F介导的信号传导和细胞增殖。INCB018424以剂量依赖性的方式显着地增加Ba/F3细胞的细胞凋亡。在Ba/F3细胞中,INCB018424(64 nM)致使线粒体去极化细胞增加一倍。INCB018424抑制来自正常捐助者和真性红细胞增多症患者的红细胞前体细胞的增殖,IC50分别是407 nM 和223 nM。 INCB018424有效抑制红细胞集落形成,IC50是67 nM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TF1 MlPYT4lv[XOnIFHzd4F6 MlP1NlAhdWmw MkLPSG1UVw>? NX\GUI13UW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKFSIMTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEWSTz3pcoR2[2WmIGPURXQ2KHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNVLPxE1? Mn\WNlI3QThyOES=
TF1 Ml\FT4lv[XOnIFHzd4F6 NEnPU|IzOCCvaX6= NFTiRnVFVVOR M3;sUmlvcGmkaYTpc44hd2ZiSlHLNUBqdiCqdX3hckBVTjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKVDZvaX7keYNm\CCVVFHUN{BxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEK0{txO NYnVOoZHOjJ4OUiwPFQ>
Human T cell NYDvfJRDU2mwYYPlJGF{e2G7 MoHXTY5pcWKrdHnvckBw\iCMQVuzM|EhcW5iaIXtZY4hXCClZXzsd{BmgHC{ZYPzbY5oKEOGMzDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFnMNk1{fGmvdXzheIVlKFOWQWS1ZUBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKz{txO M2r5[lI{PTRyNkS4
Human monocyte NU\1b2w4U2mwYYPlJGF{e2G7 NE[wXIJKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hdW:wb3P5eIV{KGW6cILld5NqdmdiQ1SxOEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGdONUOVRj3zeIlufWyjdHXkJHNVSVR3YTDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODJ4zszN NV;3WlBFOjN3NEC2OFg>
Human monocyte NWXaRXluU2mwYYPlJGF{e2G7 NET6Nm1KdmirYnn0bY9vKG:oIFrBT|IwOSCrbjDoeY1idiCvb37vZ5l1\XNiZYjwdoV{e2mwZzDDSFE1KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUU[QZ3HtcYEue3SrbYXsZZRm\CCVVFHUNUBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEOx{txO MYOyN|U1ODZ2OB?=
HEL MXzDfZRwfG:6aXOgRZN{[Xl? M3TxN|Uh|ryP NWLENndYPDhiaB?= NIPudlhEgXSxdH;4bYMhcW6mZYi9NVIvOiV? MWSyOVk{OTN2OR?=
SET-2 MV7DfZRwfG:6aXOgRZN{[Xl? MmjaOUDPxE1? NIrCTWo1QCCq MoXYR5l1d3SxeHnjJIlv\GW6PUG4Mlcm Mne1NlU6OzF|NEm=
HT93A NXnuUXhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzwcpA{OjBibl2= MmLGOUBl MYLEUXNQ M3PpZWlvcGmkaYTpc44hd2ZiR1PTMWYhcW6mdXPl[EBoemGwdXzvZ5l1cWNiZHnm[oVz\W62aXH0bY9v MnHLNlU5ODV7NkK=
CMK NGDMV25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYGyZXFGUW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIFrBT|NCPTd{VjDteZRifGmxbjDj[YxtKHC{b3zp[oVz[XSrb36= NWTqRnROOjV|NUKxNlQ>
CMK M3rqRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnQZ3Z[UW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIFrBT|NCPjOGIH31eIF1cW:wIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5zNkOg{txO NEDlT2czPTN3MkGyOC=>
CMK NWPwcFlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHX3SohKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViV2SgTmFMKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xPzVizszN M1HibFI2OzV{MUK0
NCI-H460 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTEUXNQ M{K2dWlEPTB;MD6xN{DPxE1? NWPpPJZiOjV{MUO2O|A>
NCI-H358 M1vqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{[0OWROW09? MXrJR|UxRTBwMTFOwG0> NET2NngzPTJzM{[3NC=>
A549 MnnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPEUXNQ MoezTWM2OD1yLkC0JO69VQ>? MnvjNlUzOTN4N{C=
A549/DDP M3HGNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jPS2ROW09? NVL2Xnh4UUN3ME2wMlIzKM7:TR?= NETlVIUzPTJzM{[3NC=>
NCI-H1299 NGXh[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnEUXNQ MY\JR|UxRTBwMkig{txO Mn76NlUzOTN4N{C=
NCI-H2347 NVqy[4NKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljhSG1UVw>? M4TMd2lEPTB;MD6xO{DPxE1? NUHsd2xVOjV{MUO2O|A>
A549/DDP NUP1dmFxTnWwY4Tpc44hSXO|YYm= NIDme|I{OCCwTR?= MljFOFghcA>? MnnQSG1UVw>? M3nHeWRwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? NFrsTpIzPTJzM{[3NC=>
NCI-H1299 MULGeY5kfGmxbjDBd5NigQ>? NVLNOnFOOzBibl2= MY[0PEBp MUPEUXNQ MYnEc5dvNXKnZ4XsZZRqd25ib3[gV3RCXDNicHjvd5Bpd3K7bHH0bY9v M2DMVlI2OjF|Nkew
NCI-H2347 M{DUOWZ2dmO2aX;uJGF{e2G7 Mn3tN|Ahdk1? MUW0PEBp Mo\XSG1UVw>? M1vJeGRm[3KnYYPlJIlvKEKlbEKg[ZhxemW|c3nvci=> M3XSblI2OjF|Nkew
A549/DDP NGTQSGlCeG:ydH;zbZMhSXO|YYm= MkG2N|Ahdk1? MnfjOFghcA>? MkLTSG1UVw>? NETJPJhKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NFjQOVYzPTJzM{[3NC=>
NCI-H1299 NUHPPZhYSXCxcITvd4l{KEG|c3H5 NF7pZpU{OCCwTR?= MmHrOFghcA>? MW\EUXNQ NHXIU5RKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NYTaWmJGOjV{MUO2O|A>
NCI-H2347 NGPxWHdCeG:ydH;zbZMhSXO|YYm= Ml;VN|Ahdk1? NEP2NVQ1QCCq M3LUXmROW09? NI\aXnNKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| MoDoNlUzOTN4N{C=
Hep3B NIC3eYFHfW6ldHnvckBCe3OjeR?= MoTzNUDPxE1? MUWxOkBp MnrjSG1UVw>? MVHJcZBicXKnczD0bIUh[2GyYXPpeJkhd2ZiSVjDRU1ie3OxY3nheIVlKGeyMUOwJI12fGGwdIOgeI8h[WO2aY\lJHNVSVR|IIfpeIghUUN3MDDv[kB,PTBizszN NYrvenNOOjR3MEG2PFk>
HepG2 MX7GeY5kfGmxbjDBd5NigQ>? MYKxJO69VQ>? MYSxOkBp MU\EUXNQ NU[1RmZqUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? MX:yOFUxOTZ6OR?=
Huh7 MmT2SpVv[3Srb36gRZN{[Xl? NIfr[FUyKM7:TR?= MVSxOkBp M4rNSWROW09? M3fDUGlueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyC|aXfuZYwhfG9iU2TBWFM> MU[yOFUxOTZ6OR?=
BaF3 M4S0dmtqdmG|ZTDBd5NigQ>? NFPjdGI5OCCwTR?= NFrUcm03KGh? NIDD[4RFVVOR M1LrOnJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\sLiU2TBWFUhcW5iSlHLNnY3OTeILX31eIF1\WRiQlHGN{1GWE:UIHPlcIw> M3r5WVI1OjN5N{mx
DLD-1 MUDLbY5ie2ViQYPzZZk> MXiyOUDPxE1? MWO0PEBp NVLMSYdHTE2VTx?= MYXJcohq[mm2aX;uJI9nKEqDS{GgdIhwe3Cqb4L5cIF1cW:w MX6yOFA2ODV3MB?=
RKO NUjSZ451U2mwYYPlJGF{e2G7 NUSzc5pTOjVizszN MWG0PEBp M1;3fWROW09? MmfGTY5pcWKrdHnvckBw\iCMQVuxJJBpd3OyaH;yfYxifGmxbh?= NGjGdJUzPDB3MEW1NC=>
DLD-1 NUDkSXpnU2mwYYPlJGF{e2G7 M{\6NlI2KM7:TR?= MU[0PEBp M3L4[2ROW09? MYHJcohq[mm2aX;uJI9nKEqDS{KgdIhwe3Cqb4L5cIF1cW:w MVyyOFA2ODV3MB?=
RKO NF\McnpMcW6jc3WgRZN{[Xl? M{XQOFI2KM7:TR?= Ml7zOFghcA>? NEn5RlNFVVOR MVfkc4V{KG6xdDDpcohq[mm2IFrBT|EheGixc4Doc5J6dGG2aX;u MoHYNlQxPTB3NUC=
DLD-1 NF\Q[4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljwOVAh|ryP Mof5OFghcA>? M2\UbWROW09? NHTjOlVKSzVyPUG1MlUyKM7:TR?= MX2yOFA2ODV3MB?=
RKO MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTGSY82OCEQvF2= MkLiOFghcA>? MX3EUXNQ Ml\1TWM2OD1zND63OkDPxE1? NY\nU5FSOjRyNUC1OVA>
DLD-1 NGHDUYtCeG:ydH;zbZMhSXO|YYm= M4XydFI2KM7:TR?= NIS2dFA1QCCq NGCzR2JFVVOR NGDud3RKdmS3Y3XzJIFxd3C2b4Ppd{BjgSCjY4TpeoF1cW6pIHPhd5Bie2ViMx?= MYmyOFA2ODV3MB?=
RKO NEfyT|hCeG:ydH;zbZMhSXO|YYm= M1PEc|I2KM7:TR?= M4rXe|Q5KGh? Mn\mSG1UVw>? NUTkPGZXUW6mdXPld{BieG:ydH;zbZMh[nliYXP0bZZifGmwZzDjZZNx[XOnIEO= MmT2NlQxPTB3NUC=
HuH7 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUe1NEDPxE1? Mn7EOFghcA>? NXjMbmJ[TE2VTx?= Ml7UQlgzLSC{ZXT1Z5Rqd25? NGD3cJMzOzl2MUizNi=>
SNU182 Mn7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITnb482OCEQvF2= NGXIe2k1QCCq NIT6PIRFVVOR NUf5eVFIRjZ2JTDy[YR2[3Srb36= NULEUoFbOjN7NEG4N|I>
SNU423 M17CdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDCT5M1PTBizszN M2P2UVQ5KGh? MXnEUXNQ NGezSoY,QDFnIILl[JVkfGmxbh?= MU[yN|k1OTh|Mh?=
HuH7 MlGySpVv[3Srb36gRZN{[Xl? M172[VUxKM7:TR?= M3n1WlI1KGh? MUjEUXNQ MYPJcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? NHW4RpkzOzl2MUizNi=>
SNU182 MmnoSpVv[3Srb36gRZN{[Xl? NGftOFY2OCEQvF2= MoLVNlQhcA>? Mon6SG1UVw>? MYrJcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? MoDFNlM6PDF6M{K=
SNU423 M1O4[2Z2dmO2aX;uJGF{e2G7 MkG0OVAh|ryP NIHxe3EzPCCq MkG4SG1UVw>? NUD6NFlQUW6qaXLpeIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= MlXkNlM6PDF6M{K=

... Click to View More Cell Line Experimental Data

体内研究 INCB018424(180 mg/kg,口服,每日两次)导致JAK2V617F驱动的小鼠模型的生存率在处理22天后大于90%。在JAK2V617F驱动的小鼠模型中,INCB018424(180 mg/kg,口服,每日两次)显着降低脾脏肿大和炎症因子的循环水平,并优先消灭肿瘤细胞,造成显著延长的生存期,无骨髓抑制或免疫抑制作用。[1] 在骨髓纤维化的双盲试验中,Ruxolitinib组的主要终点达到41.9%,安慰剂组则为0.7%。 Ruxolitinib导致脾体积持续减少和总症状得分提高50%或更多。[2] 在Ruxolitinib(15 mg,每天两次)组内,共28%骨髓纤维化患者至48周时脾脏体积减少至少35%,而接受最好的治疗组的比例为0%。Ruxolitinib致使脾脏长度减少了56%,而接受最好的治疗组却增加了4%。Ruxolitinib组患者的生活质量得到提高和骨髓纤维化相关症状减少。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

结合试验:

重组蛋白是使用Sf21细胞和杆状病毒载体表达的,并通过亲和层析纯化。JAK激酶测定使用肽底物(-EQEDEPEGDYFEWLE)的均相时间分辨荧光测定法。酶反应是用Ruxolitinib或对照,JAK酶,500 nM肽,三磷酸腺苷(ATP; 1mM),和2%的二甲基亚砜(DMSO)反应1小时。 50%抑制浓度(IC50)时需要抑制50%荧光信号的INCB018424浓度。
细胞实验:[1]
+ 展开
  • Cell lines: Ba/F3和HEL细胞
  • Concentrations: 3 μM
  • Incubation Time: 48小时
  • Method: 2×103细胞接种于的96孔板的一个孔中,用溶于DMSO的INCB018424(0.2%DMSO终浓度)在37℃和5% CO2条件下温育48小时。存活率是通过使用细胞滴度格洛荧光素酶试剂或活细胞计数器测定ATP水平。数值转换为相比对照的抑制百分率, IC50曲线使用Prism的GraphPad数据的非线性回归分析拟合。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: JAK2V617F驱动的小鼠模型
  • Formulation: 5%二甲基乙酰胺,0.5%methocellulose
  • Dosages: 180 mg/kg
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 61 mg/mL (199.1 mM)
Ethanol 61 mg/mL (199.1 mM)
Water Insoluble
体内 从左到右依次加入纯溶剂:
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 306.37
化学式

C17H18N6

CAS号 941678-49-5
稳定性 powder
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01712659 Recruiting T Cell Leukemia, Adult|Leukemia, Adult T-Cell|T Cell Leukemia, HTLV I Associated National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 3, 2012 Phase 2
NCT02913261 Recruiting Corticosteroid Refractory Acute Graft vs Host Disease Novartis Pharmaceuticals|Novartis February 28, 2017 Phase 3
NCT02973711 Not yet recruiting Leukemia, Chronic Myeloid University of Michigan Cancer Center February 2017 Phase 1|Phase 2
NCT03012230 Not yet recruiting Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma Mayo Clinic|National Cancer Institute (NCI) February 2017 Phase 1
NCT02928978 Not yet recruiting Ductal Carcinoma In Situ|Atypical Lobular Hyperplasia|Atypical Ductal Hyperplasia|Lobular Carcinoma In Situ Julie Nangia|Incyte Corporation|Translational Breast Cancer Research Consortium|Baylor Breast Care Center January 2017 Phase 2
NCT02966353 Not yet recruiting Primary Myelofibrosis (PMF)|Post-Polycythemia Vera-Myelofibrosis (PPV-MF)|Post-Essential Thrombocythemia Myelofibrosis (PET-MF) Novartis Pharmaceuticals|Novartis January 2017 Phase 2

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常见问题及建议解决方法

  • 问题 1:

    What is the difference between S2902 and S1378 which seem to have same structure formula according to the product information?

  • 回答:

    These two chemicals are the two different chiral forms of Ruxolitinib. S2902 S-Ruxolitinib is the S form and S1378 Ruxolitinib is the D form. One of the carbon atoms in this molecule is asymmetric, making the two molecules mirror images of each other. The biological activities of these two molecules can be very different because of the confirmation differences.

  • 问题 2:

    How about the half-life of the compound (Ruxolitinib)? How long is the duration of the inhibitory effect on JAK-STAT signaling?

  • 回答:

    The half-life of this compound in body is about 2~3 hours according to previous study. Generally, it is longer in vitro culture medium than in vivo. In paper, Ruxolitinib was also used for 24hours. http://www.bloodjournal.org/cgi/pmidlookup?view=long&pmid=24711661.

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

相关JAK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID