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39篇:

客户使用该产品的9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.

    j,k, Gene expression ofMYOCD (j) and ACTA2 ( SMA, k) after applying inhibitors of key components involved in the DDR2 downstream signalling pathway to HSCs cultured within 3D collagen matrix subjected to stretching (ST) (n=3, one-way ANOVA, **P=0.0036, ****P<0.0001). l,m, Expression of SMA was significantly reduced after treatment with related inhibitors in early-stage FμNs. (n=4, one-way ANOVA, ***P=0.001, ****P<0.0001). JAK2-i: INCB018424

    Nature Materials, 2017, 16:1252-1261.. Ruxolitinib (INCB018424) purchased from Selleck.

  • Representative images of human neutrophils from healthy controls stimulated with PMA (10 nM) after 150 min of ex vivo pretreatment with DMSO, ruxolitinib (300 nM), or GSK484 (PAD4 inhibitor,10 μM). Scale bar, 50 μm.

    Science, 2018, 10(436), doi: 10.1126/scitranslmed.aan8292. Ruxolitinib (INCB018424) purchased from Selleck.

    Scratching behavior (I), ear thickness measurement (J), representative H&E histopathology (K), and histology score (L) of vehicle control and Rux-treated mice on day 7, n R 10 mice per group. Scale bars indicate 100 mm. Data are represented as mean ± SEM.

    Cell, 2017, 171(1):217-228. 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 NXj4cVhHU2mwYYPlJGF{e2G7 M3njPVIxKG2rbh?= MX;EUXNQ Ml:0TY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJHRHOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGVRVy2rbnT1Z4VlKFOWQWS1JJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMUNOwG0> NU\XV2JtOjJ4OUiwPFQ>
TF1 NInWb4JMcW6jc3WgRZN{[Xl? NECzeXczOCCvaX6= MX3EUXNQ MYXJcohq[mm2aX;uJI9nKEqDS{GgbY4hcHWvYX6gWGYyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWw3NWmwZIXj[YQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{NN88US=> Mn;hNlI3QThyOES=
Human T cell M1O4XGtqdmG|ZTDBd5NigQ>? NH7lbppKdmirYnn0bY9vKG:oIFrBT|MwOSCrbjDoeY1idiCWIHPlcIx{KGW6cILld5NqdmdiQ1SzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwzNXO2aX31cIF1\WRiU2TBWFViKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNlPPxE1? M3zLTFI{PTRyNkS4
Human monocyte MWfLbY5ie2ViQYPzZZk> M3f1NGlvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBud26xY4n0[ZMh\XiycnXzd4lv\yCFREG0JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gS20uS1OILYP0bY12dGG2ZXSgV3RCXDWjIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOjcQvF2= MmXyNlM2PDB4NEi=
Human monocyte NF3Ge|dMcW6jc3WgRZN{[Xl? M4jlTWlvcGmkaYTpc44hd2ZiSlHLNk8yKGmwIHj1cYFvKG2xbn;jfZRmeyCneIDy[ZN{cW6pIFPENVQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKTk6pYX3tZU1{fGmvdXzheIVlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yM{JOwG0> MWqyN|U1ODZ2OB?=
HEL MlPxR5l1d3SxeHnjJGF{e2G7 NX\iS2lxPSEQvF2= M2f2XFQ5KGh? NFrsd2NEgXSxdH;4bYMhcW6mZYi9NVIvOiV? MlXvNlU6OzF|NEm=
SET-2 NWGxPFNXS3m2b4TvfIlkKEG|c3H5 M3jUdFUh|ryP M2j1XFQ5KGh? MlTKR5l1d3SxeHnjJIlv\GW6PUG4Mlcm MnToNlU6OzF|NEm=
HT93A Ml3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HCflMzOCCwTR?= M1vOeVUh\A>? MlrQSG1UVw>? NGOzT2pKdmirYnn0bY9vKG:oIFfDV{1HKGmwZIXj[YQh\3KjboXsc4N6fGmlIHTp[oZmemWwdHnheIlwdg>? MmTuNlU5ODV7NkK=
CMK NHTZdnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7EPXpKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViSlHLN2E2PzKYIH31eIF1cW:wIHPlcIwheHKxbHnm[ZJifGmxbh?= NYfDPVR2OjV|NUKxNlQ>
CMK MlGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XWbmlvcGmkaYTpc44hd2ZiQ13LJINienK7aX7nJJRp\SCMQVuzRVY{TCCvdYTheIlwdiClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvOTZ|IN88US=> NWO0UJJbOjV|NUKxNlQ>
CMK NV\1XJdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPxR2hKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViV2SgTmFMKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xPzVizszN NIrhTmgzPTN3MkGyOC=>
NCI-H460 NV7GVndPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVe4dpNmTE2VTx?= NInGbI5KSzVyPUCuNVMh|ryP NUPUcXZIOjV{MUO2O|A>
NCI-H358 NF;3WnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnifGhFVVOR MWrJR|UxRTBwMTFOwG0> NXXyZYFsOjV{MUO2O|A>
A549 M{DVT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTzWJBWTE2VTx?= NVf5S2k{UUN3ME2wMlA1KM7:TR?= NUfXT4sxOjV{MUO2O|A>
A549/DDP M{DaUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\4R4ZFVVOR NHPYbIdKSzVyPUCuNlIh|ryP NI\ZRWczPTJzM{[3NC=>
NCI-H1299 M1frb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;CZ5NFVVOR MWrJR|UxRTBwMkig{txO MUiyOVIyOzZ5MB?=
NCI-H2347 M4fQ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nLU2ROW09? Mn7vTWM2OD1yLkG3JO69VQ>? MUeyOVIyOzZ5MB?=
A549/DDP NVPob3FFTnWwY4Tpc44hSXO|YYm= NXnT[lBROzBibl2= MVu0PEBp M1\sOmROW09? MlrXSI94di2{ZXf1cIF1cW:wIH;mJHNVSVR|IIDoc5NxcG:{eXzheIlwdg>? M1;ud|I2OjF|Nkew
NCI-H1299 M1LzUmZ2dmO2aX;uJGF{e2G7 NYrtNlBDOzBibl2= NYLUT4F3PDhiaB?= M1K5[WROW09? M4LkSGRwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? M{nqe|I2OjF|Nkew
NCI-H2347 NWDUbW5NTnWwY4Tpc44hSXO|YYm= NF7ocVc{OCCwTR?= MXm0PEBp MVLEUXNQ M3OxfWRm[3KnYYPlJIlvKEKlbEKg[ZhxemW|c3nvci=> MlXZNlUzOTN4N{C=
A549/DDP NXXLN2tbSXCxcITvd4l{KEG|c3H5 MmTrN|Ahdk1? NEnWTYI1QCCq MniwSG1UVw>? M4H6R2lv\HWldHnvckBw\iCjcH;weI9{cXN? NXfmW2U3OjV{MUO2O|A>
NCI-H1299 M3n2V2Fxd3C2b4Ppd{BCe3OjeR?= M3WyVVMxKG6P M4K3WVQ5KGh? M4fsPGROW09? MlHlTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? MUSyOVIyOzZ5MB?=
NCI-H2347 M1jIO2Fxd3C2b4Ppd{BCe3OjeR?= NWPPPFVPOzBibl2= NXnwdmJbPDhiaB?= MlTRSG1UVw>? NXvXTmZzUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= M2nhSVI2OjF|Nkew
Hep3B NWPzPYVDTnWwY4Tpc44hSXO|YYm= NGi3OocyKM7:TR?= MW[xOkBp NH\TW3dFVVOR NH\QXHVKdXCjaYLld{B1cGViY3HwZYNqfHlib3[gTWhESS2jc4PvZ4lifGWmIHfwNVMxKG23dHHueJMhfG9iYXP0bZZmKFOWQWSzJJdqfGhiSVO1NEBw\iC-NUCg{txO MnvmNlQ2ODF4OEm=
HepG2 NHPUb5NHfW6ldHnvckBCe3OjeR?= M3;LfFEh|ryP MWixOkBp NXe4PVB{TE2VTx?= NX24Zo5uUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? MW[yOFUxOTZ6OR?=
Huh7 MXrGeY5kfGmxbjDBd5NigQ>? MV6xJO69VQ>? NWTv[mYyOTZiaB?= M2L3Z2ROW09? NUj5dopIUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? M1zFU|I1PTBzNki5
BaF3 Mk\TT4lv[XOnIFHzd4F6 MmixPFAhdk1? NIDEOmc3KGh? NG\0T|BFVVOR NGfacGtT\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2cEoGPURXQ2KGmwIFrBT|JXPjF5Rj3teZRifGWmIFLBSlMuTVCRUjDj[Yxt NVnzN5NkOjR{M{e3PVE>
DLD-1 NHnXW2NMcW6jc3WgRZN{[Xl? M1HyPVI2KM7:TR?= MkXnOFghcA>? MlzOSG1UVw>? NWfl[VM3UW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> MX6yOFA2ODV3MB?=
RKO MV\LbY5ie2ViQYPzZZk> M4LUdVI2KM7:TR?= MUW0PEBp MUXEUXNQ NVzNZWx[UW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> M1S0e|I1ODVyNUWw
DLD-1 NIK3bHFMcW6jc3WgRZN{[Xl? NYO2[WZJOjVizszN MU[0PEBp NWLZNHp6TE2VTx?= MkXqTY5pcWKrdHnvckBw\iCMQVuyJJBpd3OyaH;yfYxifGmxbh?= NWrCWlBKOjRyNUC1OVA>
RKO Mn\TT4lv[XOnIFHzd4F6 MkDRNlUh|ryP M4r3WlQ5KGh? MWfEUXNQ Mnv4[I9meyCwb4SgbY5pcWKrdDDKRWsyKHCqb4PwbI9zgWyjdHnvci=> NXjhRpQ2OjRyNUC1OVA>
DLD-1 NGixOGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfxbm02OCEQvF2= MnvoOFghcA>? NV7iVWxsTE2VTx?= NXm3XY9xUUN3ME2xOU42OSEQvF2= MU[yOFA2ODV3MB?=
RKO M13wZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj0TJM2OCEQvF2= MoHUOFghcA>? NWXwR|FuTE2VTx?= NUj1cpZLUUN3ME2xOE44PiEQvF2= MWSyOFA2ODV3MB?=
DLD-1 MYPBdI9xfG:|aYOgRZN{[Xl? M4fyZlI2KM7:TR?= M1XxU|Q5KGh? M3;TTGROW09? Mn;DTY5lfWOnczDhdI9xfG:|aYOgZpkh[WO2aY\heIlv\yClYYPwZZNmKDN? MXmyOFA2ODV3MB?=
RKO MVTBdI9xfG:|aYOgRZN{[Xl? Mn7RNlUh|ryP MWC0PEBp MUXEUXNQ NFjyWJJKdmS3Y3XzJIFxd3C2b4Ppd{BjgSCjY4TpeoF1cW6pIHPhd5Bie2ViMx?= MnvpNlQxPTB3NUC=
HuH7 NHXucmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV21NEDPxE1? NI\QZoE1QCCq Mn;iSG1UVw>? MXK+PFImKHKnZIXjeIlwdg>? M3n4d|I{QTRzOEOy
SNU182 MnK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofGOVAh|ryP NH7wXYs1QCCq Ml7DSG1UVw>? NVjaWWJ{RjZ2JTDy[YR2[3Srb36= NXTsbIp1OjN7NEG4N|I>
SNU423 M3rBZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO1NEDPxE1? NYXrW49bPDhiaB?= NWjueYpTTE2VTx?= MlnXQlgyLSC{ZXT1Z5Rqd25? M4\4UFI{QTRzOEOy
HuH7 MnnSSpVv[3Srb36gRZN{[Xl? MY[1NEDPxE1? M1\WelI1KGh? NEnGWFVFVVOR NF\wZpJKdmirYnn0bY9vKG:oIGPURXQyKGGwZDDTWGFVOyCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= M{DBOVI{QTRzOEOy
SNU182 NUT5THZTTnWwY4Tpc44hSXO|YYm= NEjUbIE2OCEQvF2= NUDM[5J4OjRiaB?= NGXGU2lFVVOR MX;Jcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? Mo\zNlM6PDF6M{K=
SNU423 Mn;sSpVv[3Srb36gRZN{[Xl? NUi3NG1uPTBizszN MlrGNlQhcA>? MXfEUXNQ MojYTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MYGyN|k1OTh|Mh?=

... 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 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
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
in solvent
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
NCT03041636 Recruiting Malignant Neoplasms Stated as Primary Lymphoid Haematopoietic|Other Diseases of Blood and Blood-Forming Organs|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma M.D. Anderson Cancer Center|Incyte Corporation March 8 2017 Phase 2
NCT03012230 Recruiting Breast Carcinoma Metastatic in the Bone|Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma Mayo Clinic|National Cancer Institute (NCI) December 6 2017 Phase 1
NCT02226172 Terminated Primary Myelofibrosis; Post-polycythemia Vera Myelofibrosis; Post-essential Thrombocythemia Myelofibrosis Pfizer October 6 2014 Phase 2
NCT01969838 Active not recruiting Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis Gilead Sciences December 6 2013 Phase 3
NCT03571321 Not yet recruiting Acute Lymphoblastic Leukemia|ALL Childhood|ALL University of Chicago|Incyte Corporation September 5 2019 Phase 1
NCT03616184 Recruiting Graft-versus-host-disease (GVHD) University of Nebraska September 5 2018 Phase 2

技术支持

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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