Neratinib (HKI-272)

Catalog No.S2150

Neratinib (HKI-272) Chemical Structure

Molecular Weight(MW): 557.04

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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Cited by 24 Publications

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Choose Selective HER2 Inhibitors

Biological Activity

Description 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.
Targets
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
In vitro

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT-474 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRDBwMEC1JO69VQ>? NWq0OYdYOjRyMEmwOlQ>
EFM-192A MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfDVpdiUUN3MEywMlAxPSEQvF2= NGjjNVUzPDByOUC2OC=>
HCC1569 M4rCbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTQSIlXUUN3MEywMlAxPSEQvF2= NGTjeYczPDByOUC2OC=>
HCC1954 NWfIVXlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETYSZFKSzVyPECuNFA2KM7:TR?= MWCyOFAxQTB4NB?=
MDA-MB-175 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4D5WmlEPTB:MD6wNFUh|ryP MWGyOFAxQTB4NB?=
MDA-MB-361 Mm\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRDBwMEC1JO69VQ>? M3\FNlI1ODB7ME[0
SK-BR-3 NFLpWnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvNSWVKSzVyPECuNFA2KM7:TR?= NF\wSGkzPDByOUC2OC=>
UACC-812 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRDBwMEC1JO69VQ>? MkL3NlQxODlyNkS=
UACC-893 NXLC[nI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\sOGlEPTB:MD6wNFUh|ryP MlHXNlQxODlyNkS=
SUM-225 NHPpT2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLaVnd1UUN3ME2wMlAyKM7:TR?= MX[yOFAxQTB4NB?=
SUM-190 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NICwc|NKSzVyPUCuNFEh|ryP M1K3UFI1ODB7ME[0
ZR-75-1 NWPQUmhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIS1[phKSzVyPUCuNFMh|ryP NHzIWmczPDByOUC2OC=>
HCC70 M3PvRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEm4e3FKSzVyPUCuNFMh|ryP MonFNlQxODlyNkS=
BT-20 Mn\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXDeG1KSzVyPUCuNFch|ryP NY\JZ5BYOjRyMEmwOlQ>
MDA-MB-453 M{HJbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTBwMEmg{txO NVqzRnZDOjRyMEmwOlQ>
HCC1187 MojhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX63WGxYUUN3ME2wMlExKM7:TR?= M{jYNFI1ODB7ME[0
EFM-19 Ml7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTBwMUGg{txO M3vPTFI1ODB7ME[0
T-47D NFnkVXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwMU[g{txO Ml3qNlQxODlyNkS=
MDA-MB-134 NHWxPIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jRVWlEPTB;MD6xO{DPxE1? MkPYNlQxODlyNkS=
HCC38 MknsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGT0XVBKSzVyPUCuNlUh|ryP MXqyOFAxQTB4NB?=
MDA-MB-435 NYDJc3htT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HVVmlEPTB;MD6zN{DPxE1? M2XDdFI1ODB7ME[0
MDA-MB-468 MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnhPGNQUUN3ME2wMlM{KM7:TR?= NVLPO5hnOjRyMEmwOlQ>
CAMA-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PFeGlEPTB;MD6zO{DPxE1? NFnXWnMzPDByOUC2OC=>
MDA-MB-436 M{m0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\kc4M{UUN3ME2wMlQyKM7:TR?= NGO1UYczPDByOUC2OC=>
MCF-7 MkjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\pTWM2OD1yLkSxJO69VQ>? NIexR2UzPDByOUC2OC=>
MDA-MB-415 NIezd|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\wSJpKSzVyPUCuOFIh|ryP MnX1NlQxODlyNkS=
HCC1806 NWDKV2wxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\wR2tKSzVyPUCuOFQh|ryP M3vyelI1ODB7ME[0
HCC1395 MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TpU2lEPTB;MD60PUDPxE1? M3fafFI1ODB7ME[0
HCC1937 NUfDUZZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XlT2lEPTB;MD61NEDPxE1? Mlq1NlQxODlyNkS=
HCC1143 MlK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTBwNUSg{txO MknPNlQxODlyNkS=
UACC-732 NFL6PVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPaRZFbUUN3ME2wMlY2KM7:TR?= MYCyOFAxQTB4NB?=
MDA-MB-231 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPHTWM2OD1zLkCwJO69VQ>? MVeyOFAxQTB4NB?=
MDA-MB-157 MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrqfFFjUUN3ME2xMlEzKM7:TR?= MnLnNlQxODlyNkS=
BT-549 NFrlUINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIP6SohKSzVyPUGuNVQh|ryP MmfXNlQxODlyNkS=
KPL-1 M4PUS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmW2TWM2OD1zLki5JO69VQ>? MWWyOFAxQTB4NB?=
CAL-51 NVHVZoZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEj6XmFKSzVyPUGuPFkh|ryP MUiyOFAxQTB4NB?=
BT474 MmK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorETWM2OD1yLkCwN|I{KMLzIECuNFAxPzVizszN NVrsU4N1OjN6MU[yOVQ>
SKBR3 MmKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vVbGlEPTB;MD6wNFc2KMLzIECuNFA2KM7:TR?= NIHafY8zOzhzNkK1OC=>
MDAMB453 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\ETWM2OD1zLkW5JOKyKDBwMUe5JO69VQ>? NF7rO|czOzhzNkK1OC=>
KB MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXflUYo3UUN3ME20MlE{KMLzIECuOFch|ryP MWSyNlQ6OTl|NR?=
KBv200 NXftPFJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zteWlEPTB;Nj6wN{DDuSByLk[0JO69VQ>? MWWyNlQ6OTl|NR?=
MCF-7 M3zKO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnqTWM2OD1|LkOwJOKyKDBwNEGg{txO NV\FSmNnOjJ2OUG5N|U>
MCF-7/Adr M3n4ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrR[lFmUUN3ME2gNk45QCEEsTCwMlMxKM7:TR?= MXeyNlQ6OTl|NR?=
MCF-7 M4fuemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jES2lEPTB;Mz6wNkDDuSByLkO0JO69VQ>? NWi3dlNFOjJ2OUG5N|U>
MCF-7/FLV1000 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUToRmx4UUN3ME23MlA6KMLzIECuO|Eh|ryP NYeyZ4p4OjJ2OUG5N|U>
HL60 M3T5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HVPWlEPTB;Mj6yOkDDuSByLkKzJO69VQ>? NH7nUpYzOjR7MUmzOS=>
HL60/Adr M13TcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvGZotKSzVyPUGuOFIhyrFiMD6xOUDPxE1? M4nk[FIzPDlzOUO1
HEK293/pcDNA3.1 M2\nbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\OTWM2OD13LkK5JOKyKDBwNUOg{txO MYOyNlQ6OTl|NR?=
HEK293/ABCB1 NECzfGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXKTWM2OD14LkmxJOKyKDBwN{CgJO69VQ>? NF;GO40zOjR7MUmzOS=>
SKBR MmP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\O[IUxNjBzLUGwNEBvVQ>? MlLDN{04KGR? M{\xVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M3Ltd|IyPDh5NkC1
L858R(EGFR) NEXUcm5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mojv[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MkjCNVc{OTFyMEK=
L858R/T790M(EGFR) M4rNO2NmdGxiVnnhZoltcXS7IFHzd4F6 M2LYZ4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M{LYNFE4OzFzMECy
G776insV_G/C MnrTR4VtdCCYaXHibYxqfHliQYPzZZk> NGnn[Ihl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NGW0N2kyPzNzMUCwNi=>
wild-type NILyb25E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYPk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz Mn3xNVc{OTFyMEK=
A775insYVMA Mk\4R4VtdCCYaXHibYxqfHliQYPzZZk> MnTL[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Ml:2NVc{OTFyMEK=
G776insV_G/L NX7EVINFS2WubDDWbYFjcWyrdImgRZN{[Xl? MX7k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M4DDS|E4OzFzMECy
P780insGSP NVXhV5U4S2WubDDWbYFjcWyrdImgRZN{[Xl? NFHjRlJl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NFnUOpYyPzNzMUCwNi=>
NCI-H1781 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHBUIlUcW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz Mk\RNVY5OTh4MUi=
HCC827 NInsNJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPQWlRCcW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MkDvNVY5OTh4MUi=
H3255 NV[3WGZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M33LXVE3QDF6NkG4
NCI-H1975 MnPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MWexOlgyQDZzOB?=
A549 NICyfG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrHcXdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M33oN|E3QDF6NkG4
3T3 MlnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXLTWM2OD15MECgxtEhPzhibl2= MXOxOVE4OzByOB?=
3T3/neu M{PMOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTNiwsGgNE4yPCCwTR?= NHfTR2kyPTF5M{CwPC=>
SK-Br-3 M1vkTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXCb2ttUUN3ME2yJOKyKDBwMUigcm0> NILPOVQyPTF5M{CwPC=>
BT 474 M2nlVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrzTWM2OD1{INMxJFAvODZibl2= M1WwOVE2OTd|MEC4
A431 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfSTWM2OD16MTFCtUA6KG6P NG\0TosyPTF5M{CwPC=>
MDA-MB-435 NWfuVYx7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTl4MDFCtUAyPjVibl2= NWrUenBtOTVzN{OwNFg>
SW620 M1rSfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4T3cGlEPTB;NkmwJOKyKDh2IH7N M3TrXVE2OTd|MEC4

... Click to View More Cell Line Experimental Data

Assay
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
In vivo 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]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[1]
+ Expand
  • Cell lines: 3T3, 3T3/neu, A431, BT474, SK-Br-3, MDA-MB-435, and SW480
  • Concentrations: Dissolved in DMSO, final concentrations 0.5 ng/mL-5 μg/mL
  • Incubation Time: 2 or 6 days
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Female athymic (nude) mice implanted s.c. with 3T3/neu, BT474, MCF-7, or SK-OV-3 cells
  • Formulation: Formulated in 0.5% methocellulose-0.4% polysorbate-80 (Tween 80)
  • Dosages: ~80 mg/kg/day
  • Administration: Gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL warmed (8.97 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 557.04
Formula

C30H29ClN6O3

CAS No. 698387-09-6
Storage powder
in solvent
Synonyms N/A

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  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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 Kit Metastatic Breast Cancer|Metastatic Cervical Cancer Puma Biotechnology Inc. March 14 2019 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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HER2 Signaling Pathway Map

HER2 Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID