Neratinib (HKI-272)

For research use only. Not for use in humans.

製品コードS2150

Neratinib (HKI-272)化学構造

CAS No. 698387-09-6

Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.

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HER2阻害剤の選択性比較

生物活性

製品説明 Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.
ターゲット
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
体外試験

Neratinib weakly inhibits tyrosine kinases KDR and Src with IC50 of 0.8 μM and 1.4 μM, respectively, being 14- and 24-fold less active compared with HER2. Neratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met. Neratinib selectively inhibits the proliferation of 3T3 cells transfected with the HER2 (3T3/neu), as well as two other HER-2-overexpressing SK-Br-3 and BT474 cells with IC50 values of 2-3 nM, displaying >230-fold potency compared with non-transfected 3T3 cells as well as MDA-MB-435 and SW620 which are EGFR- and HER2-negative. Neratinib also inhibits the proliferation of EGFR-dependent A431 cells with an IC50 of 81 nM. Neratinib reduces HER2 receptor autophosphorylation in BT474 cells with an IC50 of 5 nM, and EGF-dependent phosphorylation of EGFR in A431 cells with IC50 of 3 nM. Blocking of HER-2 by Neratinib results in inhibition of downstream MAPK and Akt pathways with IC50 of 2 nM, more potently than Trastuzumab. Neratinib inhibits the cyclin D1 expression and the phosphorylation of the Rb-susceptibility gene production in BT474 cells with IC50 of 9 nM, leading to G1-S arrest and ultimately decreased cell proliferation. [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT-474 MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnZWFZ7UUN3MEywMlAxPSEQvF2= MY[yOFAxQTB4NB?=
EFM-192A M{G4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRDBwMEC1JO69VQ>? NYLZUoc1OjRyMEmwOlQ>
HCC1569 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zYPWlEPTB:MD6wNFUh|ryP M3\DTFI1ODB7ME[0
HCC1954 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXCTWM2ODxyLkCwOUDPxE1? M{XuUFI1ODB7ME[0
MDA-MB-175 NXTyNpdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L3eWlEPTB:MD6wNFUh|ryP NVTXZ2xQOjRyMEmwOlQ>
MDA-MB-361 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRDBwMEC1JO69VQ>? NF;tcY8zPDByOUC2OC=>
SK-BR-3 MnvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrBTWM2ODxyLkCwOUDPxE1? MVeyOFAxQTB4NB?=
UACC-812 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTpTWM2ODxyLkCwOUDPxE1? M2[y[VI1ODB7ME[0
UACC-893 M2rJd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfpXpRKSzVyPECuNFA2KM7:TR?= M3nBPFI1ODB7ME[0
SUM-225 Mk\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DTPGlEPTB;MD6wNUDPxE1? NYDYV3g6OjRyMEmwOlQ>
SUM-190 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwMEGg{txO M1;mfFI1ODB7ME[0
ZR-75-1 Mo\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnntTWM2OD1yLkCzJO69VQ>? NXPIOmh3OjRyMEmwOlQ>
HCC70 M364WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPwTWM2OD1yLkCzJO69VQ>? MXSyOFAxQTB4NB?=
BT-20 NEHmZmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;lRmxKSzVyPUCuNFch|ryP M1HvWlI1ODB7ME[0
MDA-MB-453 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHz[5ZsUUN3ME2wMlA6KM7:TR?= NVHQd4VJOjRyMEmwOlQ>
HCC1187 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[2TWM2OD1yLkGwJO69VQ>? MUOyOFAxQTB4NB?=
EFM-19 M3LmfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjI[pAxUUN3ME2wMlEyKM7:TR?= MUSyOFAxQTB4NB?=
T-47D NVP0bYJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzVe3R4UUN3ME2wMlE3KM7:TR?= MmKxNlQxODlyNkS=
MDA-MB-134 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DYNGlEPTB;MD6xO{DPxE1? MVKyOFAxQTB4NB?=
HCC38 M2KwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:xZodKSzVyPUCuNlUh|ryP NH;GPIozPDByOUC2OC=>
MDA-MB-435 NFPz[XpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fod2lEPTB;MD6zN{DPxE1? NHLtcmQzPDByOUC2OC=>
MDA-MB-468 NInrPXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTiTWM2OD1yLkOzJO69VQ>? NU\OOWF3OjRyMEmwOlQ>
CAMA-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHaTWM2OD1yLkO3JO69VQ>? NFn5TXgzPDByOUC2OC=>
MDA-MB-436 NHzafIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXQTWM2OD1yLkSxJO69VQ>? MVKyOFAxQTB4NB?=
MCF-7 NWi4SGFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnr0TWM2OD1yLkSxJO69VQ>? MlzONlQxODlyNkS=
MDA-MB-415 NYrNTlN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M322W2lEPTB;MD60NkDPxE1? NUjObXh3OjRyMEmwOlQ>
HCC1806 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnleoRsUUN3ME2wMlQ1KM7:TR?= M1PDZlI1ODB7ME[0
HCC1395 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXn3XohRUUN3ME2wMlQ6KM7:TR?= MVmyOFAxQTB4NB?=
HCC1937 NVjwe|h6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;MXWlEPTB;MD61NEDPxE1? NUHldFJROjRyMEmwOlQ>
HCC1143 MkHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXnd|FKSzVyPUCuOVQh|ryP MUGyOFAxQTB4NB?=
UACC-732 M4O4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPBZnhNUUN3ME2wMlY2KM7:TR?= MmD2NlQxODlyNkS=
MDA-MB-231 MlL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\nOGlEPTB;MT6wNEDPxE1? MmLrNlQxODlyNkS=
MDA-MB-157 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13KOGlEPTB;MT6xNkDPxE1? MkXLNlQxODlyNkS=
BT-549 MlTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwMUSg{txO NECyT44zPDByOUC2OC=>
KPL-1 NF\JVo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTFwOEmg{txO MXeyOFAxQTB4NB?=
CAL-51 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfKTWM2OD1zLki5JO69VQ>? NYHVfVl7OjRyMEmwOlQ>
BT474 Ml7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LhemlEPTB;MD6wNFMzOyEEsTCwMlAxODd3IN88US=> MWOyN|gyPjJ3NB?=
SKBR3 NEW5dmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwMEC3OUDDuSByLkCwOUDPxE1? NHzHTGozOzhzNkK1OC=>
MDAMB453 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTFwNUmgxtEhOC5zN{mg{txO MmnuNlM5OTZ{NUS=
KB MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rtNGlEPTB;ND6xN{DDuSByLkS3JO69VQ>? NF;nfXEzOjR7MUmzOS=>
KBv200 M2X0b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXlfmhKSzVyPU[uNFMhyrFiMD62OEDPxE1? NIrwZngzOjR7MUmzOS=>
MCF-7 MknQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHuTWM2OD1|LkOwJOKyKDBwNEGg{txO NVuwW4cyOjJ2OUG5N|U>
MCF-7/Adr NUnHZlljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRSB{Lki4JOKyKDBwM{Cg{txO MVWyNlQ6OTl|NR?=
MCF-7 NVr2Om9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvveI1KSzVyPUOuNFIhyrFiMD6zOEDPxE1? MmLtNlI1QTF7M{W=
MCF-7/FLV1000 MkTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\TSIFQUUN3ME23MlA6KMLzIECuO|Eh|ryP NFTKeXAzOjR7MUmzOS=>
HL60 NVLo[okyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;Dd3ZoUUN3ME2yMlI3KMLzIECuNlMh|ryP MVqyNlQ6OTl|NR?=
HL60/Adr MkLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPYcI1KSzVyPUGuOFIhyrFiMD6xOUDPxE1? MXyyNlQ6OTl|NR?=
HEK293/pcDNA3.1 NHnrb4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTuTWM2OD13LkK5JOKyKDBwNUOg{txO NGO2UHYzOjR7MUmzOS=>
HEK293/ABCB1 MnLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HYb2lEPTB;Nj65NUDDuSByLkewJEDPxE1? M13KfFIzPDlzOUO1
SKBR M3u4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVr0cmVxOC5yMT2xNFAhdk1? MWizMVch\A>? NIfJemhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> Moi2NlE1QDd4MEW=
L858R(EGFR) NULU[md1S2WubDDWbYFjcWyrdImgRZN{[Xl? MVvk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MXKxO|MyOTByMh?=
L858R/T790M(EGFR) Mo\IR4VtdCCYaXHibYxqfHliQYPzZZk> Mo\T[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MVSxO|MyOTByMh?=
G776insV_G/C Mn76R4VtdCCYaXHibYxqfHliQYPzZZk> NGnWTHBl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MYmxO|MyOTByMh?=
wild-type NWfIe25GS2WubDDWbYFjcWyrdImgRZN{[Xl? M4\pUIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NWPxenVqOTd|MUGwNFI>
A775insYVMA NVvHfYRtS2WubDDWbYFjcWyrdImgRZN{[Xl? NHTZV3Rl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M3HaWFE4OzFzMECy
G776insV_G/L MXjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXTRPHhC\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MoPwNVc{OTFyMEK=
P780insGSP MnrhR4VtdCCYaXHibYxqfHliQYPzZZk> MX;k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NHz6THcyPzNzMUCwNi=>
NCI-H1781 NGf1ZZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= Mkj5NVY5OTh4MUi=
HCC827 NFjtNmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVz6foxpcW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MlzZNVY5OTh4MUi=
H3255 MmLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= Ml\QNVY5OTh4MUi=
NCI-H1975 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLVR2t2cW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz Mlz2NVY5OTh4MUi=
A549 NXPvfFZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\vOIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MoO3NVY5OTh4MUi=
3T3 NU\yZY9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fkSWlEPTB;N{CwJOKyKDd6IH7N M{S4dFE2OTd|MEC4
3T3/neu MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTNiwsGgNE4yPCCwTR?= Ml20NVUyPzNyMEi=
SK-Br-3 NYO1UZQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPHTWM2OD1{INMxJFAvOThibl2= M3LtTFE2OTd|MEC4
BT 474 M1G4OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmW1TWM2OD1{INMxJFAvODZibl2= NXvPWZdoOTVzN{OwNFg>
A431 M4nlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnq5TWM2OD16MTFCtUA6KG6P NUXmdm5IOTVzN{OwNFg>
MDA-MB-435 NV3yfZI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTl4MDFCtUAyPjVibl2= NHXVU2gyPTF5M{CwPC=>
SW620 M3LlZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDXTWM2OD14OUCgxtEhQDRibl2= NWrCVIhXOTVzN{OwNFg>

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アッセイ
Methods Test Index PMID
Western blot
pHER2 / HER2 / pAKT / AKT / pERK / ERK ; 

PubMed: 24009064     


BT474 (right) and SKBR3 (left) cell were treated for 1 hour or 1 day with increasing concentrations of neratinib. After lysis, protein levels were assessed using western blotting techniques.

p-ERBB2 / ERBB2 / p-ERBB3 / ERBB3 / p-EGFR / p-90RSK ; 

PubMed: 30118499     


(A) Effects of MEK162 alone, neratinib alone, and the combination of MEK162 plus neratinib were assessed in sensitive, inflammatory subtype cell lines (NCI-H747, SW-837), (B) resistant, stem-like subtype cell lines (SW480, SW620). Cell lines were cultured䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뙠ෆ䐺痖暼瘿뙠ෆᾰƌ 뙠ෆÐ㺣痖뙠ෆ€𢡄뙤ෆ€䀷痗뙤ෆ౴뙤ෆ㵶痗뙤ෆ뺖᎒泌Itemセ᎒

24009064 30118499
Growth inhibition assay
Cell viability ; 

PubMed: 30118499     


NCI-H747, SW837, SW1116, SW1463, NCI-H508, SNU-C1, SW480, SW620, C2BBE1, Hs675.T, and HCT116 cells were treated with a constant dose of MEK162 (0.5 μM) in combination with different doses of neratinib for 72 hours. Dimethyl sulfoxide (DMSO) (0.01%) was us䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒

30118499
体内試験 Oral administration of Neratinib significantly inhibits the growth of 3T3/neu xenografts, with inhibition of 34%, 53%, 98%, and 98% at dose of 10, 20, 40, and 80 mg/kg/day, respectively. Consistent with the inhibition of HER-2 phosphorylation by 84% within 1 hour of administration at 40 mg/kg/day, Neratinib inhibits the growth of BT474 xenografts by 70-82%, 67%, and 93% at dose of 5, 10, and 40 mg/kg/day, respectively. Neratinib is also effective against SK-OV-3 xenografts with inhibition of 31% and 85% at 5 and 60 mg/kg/day, respectively. Neratinib is less potent against EGFR-dependent A431 xenografts than HER-2-dependent tumors, with 32% and 44% inhibition at 5 and 20 mg/kg/day, respectively. Neratinib displays little activity against MCF-7 and MX-1 xenografts expressing low levels of HER-2 and EGFR, with only 28% inhibition at 80 mg/kg/day, suggesting that Neratinib has selective activity for cells expressing HER-2 or EGFR. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
- 合併

Cell-free autophosphorylation assay using time-resolved fluorometry:

Neratinib is prepared as 10 mg/mL stocks in DMSO and diluted in 25 mM HEPES (pH 7.5; 0.002 ng/mL-20 μg/mL). Purified recombinant COOH-terminal fragments of HER2 (amino acids 676-1255) or epidermal growth factor receptor (EGFR) (amino acids 645-1186) [diluted in 100 mM HEPES (pH 7.5) and 50% glycerol] is incubated with increasing concentrations of Neratinib in 4 mM HEPES (pH 7.5), 0.4 mM MnCl2, 20 μM sodium vanadate, and 0.2 mM DTT for 15 minutes at room temperature in 96-well ELISA plates. The kinase reaction is initiated by the addition of 40 μM ATP and 20 mM MgCl2 and allowed to proceed for 1 hour at room temperature. Plates are washed, and phosphorylation is detected using Europium-labeled anti-phospho-tyrosine antibodies (15 ng/well). After washing and enhancement steps, signal is detected using a Victor2 fluorescence reader (excitation wavelength 340 nm, emission wavelength 615 nm). The concentration of Neratinib that inhibits receptor phosphorylation by 50% (IC50) is calculated from inhibition curves.
細胞試験: [1]
- 合併
  • 細胞株: 3T3, 3T3/neu, A431, BT474, SK-Br-3, MDA-MB-435, and SW480
  • 濃度: Dissolved in DMSO, final concentrations 0.5 ng/mL-5 μg/mL
  • 反応時間: 2 or 6 days
  • 実験の流れ: Cells are exposed to various concentrations of Neratinib for 2, or 6 days. Cell proliferation is determined using sulforhodamine B, a protein binding dye. Briefly, cells are fixed with 10% trichloroacetic acid and washed extensively with water. Cells are then stained with 0.1% sulforhodamine B and washed in 5% acetic acid. Protein-associated dye is solubilized in 10 mM Tris, and absorbance is measured at 450 nM. The concentration of Neratinib that inhibits cell proliferation by 50% (IC50) is determined from inhibition curves.
    (参考用のみ)
動物試験:[1]
- 合併
  • 動物モデル: Female athymic (nude) mice implanted s.c. with 3T3/neu, BT474, MCF-7, or SK-OV-3 cells
  • 投薬量: ~80 mg/kg/day
  • 投与方法: Gavage
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 5 mg/mL (8.97 mM) warming
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% PEG400+0.5% Tween80+5% propylene glycol
混合させたのち直ちに使用することを推奨します。
5 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 557.04
化学式

C30H29ClN6O3

CAS No. 698387-09-6
Storage powder
in solvent
別名 N/A
Smiles CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CCN(C)C

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04388384 Recruiting Drug: Neratinib Breast Neoplasm Pierre Fabre Pharma GmbH|iOMEDICO AG|Pierre Fabre Pharma Austria|Pierre Fabre Pharma AG April 20 2020 --
NCT03812393 Recruiting Drug: Neratinib Triple Negative Breast Cancer|Early-stage Breast Cancer|HER2-positive Breast Cancer West Cancer Center|Celcuity|Puma Biotechnology Inc. June 21 2019 Phase 2
NCT03919292 Recruiting Drug: Neratinib|Drug: Divalproex Sodium Solid Tumor Adult Virginia Commonwealth University|Puma Biotechnology Inc. May 1 2019 Phase 1|Phase 2
NCT03786107 Recruiting Diagnostic Test: Almac HER-Seq Assay Hormone Receptor-Positive HER2-Negative Metastatic Breast Cancer|Metastatic Cervical Cancer Puma Biotechnology Inc. March 14 2019 --

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

HER2シグナル伝達経路

HER2 Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID