Neratinib (HKI-272)

目录号:S2150

Neratinib (HKI-272) Chemical Structure

Molecular Weight(MW): 557.04

Neratinib (HKI-272)是一种高度选择性的HER2EGFR抑制剂,在无细胞试验中IC50分别为59 nM 和 92 nM;微弱抑制KDR和Src,对Akt,CDK1/2/4,IKK-2,MK-2,PDK1,c-Raf和c-Met没有显著的抑制作用。Phase 3。

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RMB 7933.43 现货
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客户使用该产品的5个实验数据:

  •  

    Differential sensitivity of EGFR-mutant glioma and lung cancer cell lines to the irreversible EGFR inhibitors HKI-272 and CI-1033. C, HKI-272 is more potent than CI-1033 in blocking EGFR phosphorylation in SKMG3 cells with EGFR EC mutation. SKMG3 cells were treated with the indicated doses of CI-1033 or HKI-272, and whole lysates were analyzed by immunoblot with the indicated antibodies.

    Cancer Discov 2012 2, 458-471. Neratinib (HKI-272) purchased from Selleck.

     

    Differential sensitivity of EGFR-mutant glioma and lung cancer cell lines to the irreversible EGFR inhibitors HKI-272 and CI-1033. A, HKI-272 induces cell death in GBM cells with EGFR EC mutation (SKMG3, SF268) but not EGFR wild-type (WT EGFR) cancer cell lines or astrocytes (NHA). Cell death was assessed by trypan blue exclusion after 5 days of inhibitor treatment. Cells lines in black express wild-type EGFR, whereas those in red contain EGFR EC mutations.

    Cancer Discov 2012 2, 458-471. Neratinib (HKI-272) purchased from Selleck.

  • HER2 mutations V777L, D769H, V842I, G309A induce gain-of-function over HER2 WT in MCF10A mammary epithelial cells. B, HER2 WT, L755S, and del.755–759 cells were grown in Matrigel in the presence of DMSO vehicle (0.5%), neratinib (0.5  μmol/L) or gefitinib (0.5  μmol/L). Phase contrast images were obtained as in A. C,  MCF10A-HER2 WT or mutants were seeded in soft agar. After 7 days of growth, they were treated with DMSO vehicle (0.5%), lapatinib (0.5 μmol/L) or neratinib (0.5 μmol/L) for an additional week. Error bars represent 95% highest posterior density intervals. *, Significant difference between the HER2 mutant and HER2 WT; #, the effect of inhibitor treatment was significant (95% highest posterior density interval did not contain 0 for both).  D, photomicrographs of the colonies in soft agar on day 12, magnification ×40. 

    Cancer Discov 2013 3, 224-37. Neratinib (HKI-272) purchased from Selleck.

    (C, D) Cells were treated as mentioned above for the indicated times and processed for immunofluorescence experiments with anti-ErbB2 antibody (green). Nuclei were stained with DAPI (blue). Examples of intracellular ErbB2 punctae are indicated with yellow triangles. Scale bar = 10 μm.

    Cancer Lett, 2016, 382(2):176-185. Neratinib (HKI-272) purchased from Selleck.

  • Mean IC50 value of Neratinib. *IC50 is the mean concentration of drug that reduced cell survival by 50% in at least two experiments. Data are shown as mean ± SD (n=6) of one representative experiment. Similar results were obtained in three experiments. *p < 0.05; **p < 0.01;*** p < 0.001

    Oncotarget, 2016, 7(36):58038-58050. Neratinib (HKI-272) purchased from Selleck.

产品安全说明书

HER2抑制剂选择性比较

生物活性

产品描述 Neratinib (HKI-272)是一种高度选择性的HER2EGFR抑制剂,在无细胞试验中IC50分别为59 nM 和 92 nM;微弱抑制KDR和Src,对Akt,CDK1/2/4,IKK-2,MK-2,PDK1,c-Raf和c-Met没有显著的抑制作用。Phase 3。
靶点
HER2 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
KDR [1]
(Cell-free assay)
Src [1]
(Cell-free assay)
59 nM 92 nM 800 nM 1.4 μM
体外研究

Neratinib微弱抑制酪氨酸激酶KDR 和Src,IC50分别为0.8 μM 和 1.4 μM,与 HER-2相比,活性分别弱14和24倍。Neratinib 作用于其他丝-苏氨酸激酶如Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, 和Tpl-2,以及酪氨酸激酶c-Met没有活性。Neratinib选择性抑制转染 HER-2 (3T3/neu)的3T3细胞增殖,也抑制两种其他 HER-2-过表达的SK-Br-3和 BT474 cells细胞增殖,IC50为 2-3 nM,与未转染的3T3细胞及 EGFR-和 HER-2阴性的MDA-MB-435 和 SW620细胞相比,效果高230倍以上。Neratinib也抑制EGFR-依赖的A431细胞增殖,IC50为81 nM。Neratinib 作用于BT474 细胞,降低HER-2受体自磷酸化, IC50 为5 nM,作用于A431细胞,降低EGF依赖的 EGFR磷酸化,IC50 为3 nM。Neratinib抑制 HER-2,导致下游MAPK和Akt通路受抑制,IC50为2 nM,比Trastuzumab更有效。Neratinib 作用于BT474细胞,抑制cyclin D1表达和 Rb-敏感性基因产物的磷酸化,IC50为9 nM,导致细胞周期停在G1-S期,最终降低细胞增殖。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT-474 NIHvS4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{CxW2lEPTB:MD6wNFUh|ryP NYL2eoxzOjRyMEmwOlQ>
EFM-192A NXXwTJFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\GUllKSzVyPECuNFA2KM7:TR?= NF\n[2kzPDByOUC2OC=>
HCC1569 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjr[GdQUUN3MEywMlAxPSEQvF2= MYKyOFAxQTB4NB?=
HCC1954 NHf3O4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLoTWM2ODxyLkCwOUDPxE1? NU\mbJM1OjRyMEmwOlQ>
MDA-MB-175 NE[5WG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRDBwMEC1JO69VQ>? NILPOZMzPDByOUC2OC=>
MDA-MB-361 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELHVpNKSzVyPECuNFA2KM7:TR?= MVyyOFAxQTB4NB?=
SK-BR-3 MmXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DiXmlEPTB:MD6wNFUh|ryP MlTBNlQxODlyNkS=
UACC-812 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRDBwMEC1JO69VQ>? M{i1dVI1ODB7ME[0
UACC-893 Mo\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkizTWM2ODxyLkCwOUDPxE1? MV2yOFAxQTB4NB?=
SUM-225 MkKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjRTWM2OD1yLkCxJO69VQ>? NFnPW3MzPDByOUC2OC=>
SUM-190 M{nwZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknhTWM2OD1yLkCxJO69VQ>? M{m3e|I1ODB7ME[0
ZR-75-1 M4\RPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\hRYM6UUN3ME2wMlA{KM7:TR?= NH;YS3gzPDByOUC2OC=>
HCC70 NVvrXGNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTBwMEOg{txO MonkNlQxODlyNkS=
BT-20 NIPkVY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3X6TmlEPTB;MD6wO{DPxE1? M{Lad|I1ODB7ME[0
MDA-MB-453 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\OTWM2OD1yLkC5JO69VQ>? NGrOb4UzPDByOUC2OC=>
HCC1187 M{fjVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jZe2lEPTB;MD6xNEDPxE1? MoWxNlQxODlyNkS=
EFM-19 NX3afWhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTBwMUGg{txO MYmyOFAxQTB4NB?=
T-47D MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTRS2MyUUN3ME2wMlE3KM7:TR?= M1;NeFI1ODB7ME[0
MDA-MB-134 NHHM[GtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzBS41xUUN3ME2wMlE4KM7:TR?= MYWyOFAxQTB4NB?=
HCC38 NGHObFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PIcGlEPTB;MD6yOUDPxE1? NFjKOJczPDByOUC2OC=>
MDA-MB-435 MkHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXR[3BkUUN3ME2wMlM{KM7:TR?= NEHyWZMzPDByOUC2OC=>
MDA-MB-468 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwM{Og{txO NWjrOG53OjRyMEmwOlQ>
CAMA-1 NYL1TmFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\ob2ZWUUN3ME2wMlM4KM7:TR?= Ml;QNlQxODlyNkS=
MDA-MB-436 NGDRZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3KdnZtUUN3ME2wMlQyKM7:TR?= NXLKdGt5OjRyMEmwOlQ>
MCF-7 NV\yU|VxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH5[oNVUUN3ME2wMlQyKM7:TR?= Mk\6NlQxODlyNkS=
MDA-MB-415 MoHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrHV5BKSzVyPUCuOFIh|ryP M37NPFI1ODB7ME[0
HCC1806 NHjiWHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwNESg{txO M1K4e|I1ODB7ME[0
HCC1395 NHPqVoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjNdW9KSzVyPUCuOFkh|ryP NF;GfFUzPDByOUC2OC=>
HCC1937 M1vhSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnviTWM2OD1yLkWwJO69VQ>? M1nDe|I1ODB7ME[0
HCC1143 NUHPWXV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTBwNUSg{txO NWrkUXFzOjRyMEmwOlQ>
UACC-732 NYPGeIYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTBwNkWg{txO M3vnZlI1ODB7ME[0
MDA-MB-231 NVrSWnJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFwMECg{txO NGX2S5UzPDByOUC2OC=>
MDA-MB-157 M1Kzdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIj1cmtKSzVyPUGuNVIh|ryP M{fn[FI1ODB7ME[0
BT-549 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTFwMUSg{txO MXKyOFAxQTB4NB?=
KPL-1 M1G1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTFwOEmg{txO NVv5PHlzOjRyMEmwOlQ>
CAL-51 NWPKeFJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXjTWM2OD1zLki5JO69VQ>? NEjaOWYzPDByOUC2OC=>
BT474 NIrrUWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvOSIp7UUN3ME2wMlAxOzJ|INMxJFAvODByN{Wg{txO M2TiWVI{QDF4MkW0
SKBR3 M4PN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7JTWM2OD1yLkCwO|UhyrFiMD6wNFUh|ryP MY[yN|gyPjJ3NB?=
MDAMB453 MnPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEm0VGlKSzVyPUGuOVkhyrFiMD6xO|kh|ryP MnHWNlM5OTZ{NUS=
KB M3fXOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnn5TWM2OD12LkGzJOKyKDBwNEeg{txO NWf5OnBUOjJ2OUG5N|U>
KBv200 NYTDNHlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLE[I9MUUN3ME22MlA{KMLzIECuOlQh|ryP M{DKd|IzPDlzOUO1
MCF-7 MknZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TPPGlEPTB;Mz6zNEDDuSByLkSxJO69VQ>? M{e3TlIzPDlzOUO1
MCF-7/Adr MkPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jLSmlEPTB;IEKuPFghyrFiMD6zNEDPxE1? M1:2cFIzPDlzOUO1
MCF-7 NYnMZY9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTNwMEKgxtEhOC5|NDFOwG0> MmPRNlI1QTF7M{W=
MCF-7/FLV1000 NFWze21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLwW4lMUUN3ME23MlA6KMLzIECuO|Eh|ryP NYrkdJZOOjJ2OUG5N|U>
HL60 MonoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTJwMk[gxtEhOC5{MzFOwG0> NUPUVlN6OjJ2OUG5N|U>
HL60/Adr NWjPSlRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TkNWlEPTB;MT60NkDDuSByLkG1JO69VQ>? NGnR[HMzOjR7MUmzOS=>
HEK293/pcDNA3.1 M4rvT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fQ[WlEPTB;NT6yPUDDuSByLkWzJO69VQ>? MXKyNlQ6OTl|NR?=
HEK293/ABCB1 NWXrbI1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1v3VmlEPTB;Nj65NUDDuSByLkewJEDPxE1? NHPlSGwzOjR7MUmzOS=>
SKBR MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\ud|AvODFvMUCwJI5O M{juVFMuPyCm MVfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NH30UogzOTR6N{[wOS=>
L858R(EGFR) M13nXGNmdGxiVnnhZoltcXS7IFHzd4F6 M3PJfIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NWLmTYxOOTd|MUGwNFI>
L858R/T790M(EGFR) NXLXfJNFS2WubDDWbYFjcWyrdImgRZN{[Xl? M2nRW4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MUGxO|MyOTByMh?=
G776insV_G/C Ml6yR4VtdCCYaXHibYxqfHliQYPzZZk> MnjK[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHzUeFMyPzNzMUCwNi=>
wild-type NV;MNYJmS2WubDDWbYFjcWyrdImgRZN{[Xl? M{ThbIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NGC4PIIyPzNzMUCwNi=>
A775insYVMA MlzxR4VtdCCYaXHibYxqfHliQYPzZZk> NEnUPJdl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NYLCfIpPOTd|MUGwNFI>
G776insV_G/L MkfhR4VtdCCYaXHibYxqfHliQYPzZZk> NVixfFAz\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M2OyT|E4OzFzMECy
P780insGSP NFv6To1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NI[zcYhl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MUexO|MyOTByMh?=
NCI-H1781 NVjET4dET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;qSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NH:5fnEyPjhzOE[xPC=>
HCC827 NIfLOHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M2jobFE3QDF6NkG4
H3255 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIH2SlBqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NFXEU4kyPjhzOE[xPC=>
NCI-H1975 M1vZUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NECxOm9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M4\OdVE3QDF6NkG4
A549 Ml;sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MoPsNVY5OTh4MUi=
3T3 NUnlfJJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnm4TWM2OD15MECgxtEhPzhibl2= M4jFZlE2OTd|MEC4
3T3/neu M3Px[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS3TWM2OD1|INMxJFAvOTRibl2= MYKxOVE4OzByOB?=
SK-Br-3 Mn7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHUU49KSzVyPUKgxtEhOC5zODDuUS=> MXWxOVE4OzByOB?=
BT 474 NWT6RXM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJiwsGgNE4xPiCwTR?= NXXSTGV4OTVzN{OwNFg>
A431 NF:3enFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PGb2lEPTB;OEGgxtEhQSCwTR?= NISydo8yPTF5M{CwPC=>
MDA-MB-435 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PtdWlEPTB;OU[wJOKyKDF4NTDuUS=> MlWyNVUyPzNyMEi=
SW620 NWn1RldsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\2TXljUUN3ME22PVAhyrFiOESgcm0> MX6xOVE4OzByOB?=

... Click to View More Cell Line Experimental Data

体内研究 Neratinib每天按10, 20, 40, 和80 mg/kg剂量口服处理给药3T3/neu 移植瘤,显著抑制生长,分别抑制34%, 53%, 98%, 和 98%。Neratinib每天按40 mg/kg剂量处理,1小时内抑制 84% HER-2磷酸化,相应地,Neratinib 每天按5, 10, 和 40 mg/kg剂量处理BT474 移植瘤,抑制分别为70-82%, 67%, 和 93%。Neratinib也有效作用于SK-OV-3移植瘤,每天按 5 和 60 mg/kg剂量处理,抑制分别为 31% 和85% 。Neratinib作用于EGFR依赖性A431移植瘤比作用于HER-2-依赖性肿瘤效果弱, 每天按5 和 20 mg/kg剂量处理,抑制分别为32%和44%。Neratinib作用于表达低水平HER-2和EGFR的MCF-7和 MX-1移植瘤几乎没有活性, 每天按80 mg/kg剂量处理抑制只为28%,说明Neratinib 选择性作用于表达HER-2或EGFR的细胞。[1]

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]
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使用时间-分辨荧光分析无细胞自磷酸化:

Neratinib 在DMSO 中制备成10 mg/mL 储液,然后在25 mM HEPES (pH 7.5; 0.002 ng/mL-20 μg/mL)中稀释。纯化重组的HER-2 COOH末端片段(第676-1255位氨基酸) 或EGFR COOH末端片段(第 645-1186位氨基酸)[在100 mM HEPES (pH 7.5) 和50% 甘油中稀释] 与浓度不断增高的Neratinib 在96-孔ELISA板上室温下温育15分钟,孔中含4 mM HEPES (pH 7.5), 0.4 mM MnCl2, 20 μM 钒酸钠,及 0.2 mM DTT 。加入 40 μM ATP 和20 mM MgCl2开始激酶反应,然后在室温下反应1小时。冲洗实验板, 使用铕标记的抗-磷酸化-酪氨酸抗体 (15 ng/每孔)检测磷酸化。冲洗后,使用Victor2 荧光读数仪 (激发波长为340 nm,发射波长为615 nm)测定信号。通过抑制曲线测定抑50%受体磷酸时的Neratinib 浓度 (IC50) 。
细胞实验:[1]
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  • Cell lines: 3T3, 3T3/neu, A431, BT474, SK-Br-3, MDA-MB-435, 和SW480
  • Concentrations: 溶于DMSO, 终浓度为0.5 ng/mL-5 μg/mL
  • Incubation Time: 2, 或6天
  • Method: 使用不同浓度Neratinib处理细胞 2, 或6 天。使用sulforhodamine B, 一种蛋白结合染料,测定细胞增殖。细胞与10% 三氯乙酸混合,然后使用水广泛冲洗。使用 0.1% sulforhodamine B对细胞进行染色,使用在5% 乙酸中清洗。蛋白-结合染10 mM Tris中,然后在450 nM处测定吸光度。通过抑制曲线测定抑制50% 细胞增殖时的Neratinib 浓度(IC50)。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 皮下移植3T3/neu, BT474, MCF-7, 或 SK-OV-3 细胞的雌性无胸腺裸鼠
  • Formulation: 在0.5% 甲基纤维素-0.4% Tween--80 (Tween-80)中配制
  • Dosages: ~80 mg/kg/day
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 5 mg/mL warmed (8.97 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用:
30% PEG400+0.5% Tween80+5% propylene glycol
5 mg/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 557.04
化学式

C30H29ClN6O3

CAS号 698387-09-6
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
NCT02977780 Recruiting Glioblastoma Dana-Farber Cancer Institute|Eli Lilly and Company|Celgene|Puma Biotechnology, Inc.|Accelerate Brain Cancer Cure February 9, 2017 Phase 2
NCT02673398 Recruiting HER2 Positive Breast Carcinoma|Recurrent Breast Carcinoma|Stage IV Breast Cancer City of Hope Medical Center|National Cancer Institute (NCI)|Puma Biotechnology, Inc. October 2016 Phase 2
NCT02932280 Recruiting Solid Tumor|Central Nervous System Tumor|Lymphoma|Leukemia Memorial Sloan Kettering Cancer Center|Milton S. Hershey Medical Center|M.D. Anderson Cancer Center|Stanford University|Arkansas Childrens Hospital Research Institute|Alberta Childrens Hospital|Phoenix Childrens Hospital|University of Texas October 2016 Phase 1|Phase 2
NCT02593708 Recruiting Solid Tumor Michelle Melisko|University of California, San Francisco October 2015 Phase 1
NCT02400476 Recruiting Early Stage HER2+ Breast Cancer Puma Biotechnology, Inc. February 2015 Phase 2
NCT02236000 Recruiting Breast Cancer NSABP Foundation Inc|Puma Biotechnology, Inc. August 2014 Phase 1|Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID