Neratinib (HKI-272)

For research use only. Not for use in humans.

Catalog No.S2150

41 publications

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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Selleck's Neratinib (HKI-272) has been cited by 41 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 MoDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33PWGlEPTB:MD6wNFUh|ryP M4\WTlI1ODB7ME[0
EFM-192A NYXK[YhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfKTWM2ODxyLkCwOUDPxE1? MXWyOFAxQTB4NB?=
HCC1569 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LPXGlEPTB:MD6wNFUh|ryP M{j3c|I1ODB7ME[0
HCC1954 MnHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfCTWM2ODxyLkCwOUDPxE1? NWXTSIl2OjRyMEmwOlQ>
MDA-MB-175 MlPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRDBwMEC1JO69VQ>? MnroNlQxODlyNkS=
MDA-MB-361 M1TXTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXHNpNKSzVyPECuNFA2KM7:TR?= MU[yOFAxQTB4NB?=
SK-BR-3 M{PKfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\KXGRYUUN3MEywMlAxPSEQvF2= Ml3qNlQxODlyNkS=
UACC-812 MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\pe3BKUUN3MEywMlAxPSEQvF2= Ml;LNlQxODlyNkS=
UACC-893 M2TlUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrPcHlxUUN3MEywMlAxPSEQvF2= MWCyOFAxQTB4NB?=
SUM-225 NVn3NXgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3WyNWlEPTB;MD6wNUDPxE1? M33ZdFI1ODB7ME[0
SUM-190 NV;nT|ZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;seHlKSzVyPUCuNFEh|ryP NYTKO2xnOjRyMEmwOlQ>
ZR-75-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwMEOg{txO MlK3NlQxODlyNkS=
HCC70 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTBwMEOg{txO MkTyNlQxODlyNkS=
BT-20 Ml;pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwMEeg{txO MkjVNlQxODlyNkS=
MDA-MB-453 NXfES5oxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXmdXZ6UUN3ME2wMlA6KM7:TR?= NGn3NZYzPDByOUC2OC=>
HCC1187 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XXSmlEPTB;MD6xNEDPxE1? NHP6XoMzPDByOUC2OC=>
EFM-19 NEHvcW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nRNmlEPTB;MD6xNUDPxE1? NFnTU|YzPDByOUC2OC=>
T-47D NGXFdYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrwS3NKSzVyPUCuNVYh|ryP NX[xW4dqOjRyMEmwOlQ>
MDA-MB-134 NUPIOmNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnWTWM2OD1yLkG3JO69VQ>? M4DU[lI1ODB7ME[0
HCC38 NHjPWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfWTWM2OD1yLkK1JO69VQ>? NHmzPXQzPDByOUC2OC=>
MDA-MB-435 NWK0XIl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwM{Og{txO MXiyOFAxQTB4NB?=
MDA-MB-468 NEHYe4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz6TWM2OD1yLkOzJO69VQ>? MYSyOFAxQTB4NB?=
CAMA-1 NV\EfIRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T5e2lEPTB;MD6zO{DPxE1? NELMRmkzPDByOUC2OC=>
MDA-MB-436 NIPZSnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInNcYlKSzVyPUCuOFEh|ryP MoXKNlQxODlyNkS=
MCF-7 NH7qWJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwNEGg{txO M{jLPVI1ODB7ME[0
MDA-MB-415 NIH1UVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LP[WlEPTB;MD60NkDPxE1? M3fpZlI1ODB7ME[0
HCC1806 M37Zbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTMSVVXUUN3ME2wMlQ1KM7:TR?= MYGyOFAxQTB4NB?=
HCC1395 NXzYeWFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUX1VIJuUUN3ME2wMlQ6KM7:TR?= NIn6cHAzPDByOUC2OC=>
HCC1937 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnqZplKSzVyPUCuOVAh|ryP NIjy[ngzPDByOUC2OC=>
HCC1143 NYHhUVc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVm4OIRZUUN3ME2wMlU1KM7:TR?= M2njcFI1ODB7ME[0
UACC-732 NHS2R3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWSw[4VrUUN3ME2wMlY2KM7:TR?= MnrjNlQxODlyNkS=
MDA-MB-231 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTFwMECg{txO M332cVI1ODB7ME[0
MDA-MB-157 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v5bmlEPTB;MT6xNkDPxE1? NVf1S|dLOjRyMEmwOlQ>
BT-549 M3v6dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLCcZNKSzVyPUGuNVQh|ryP NHu2U2szPDByOUC2OC=>
KPL-1 M1\5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDZXZFKSzVyPUGuPFkh|ryP M1P3RVI1ODB7ME[0
CAL-51 MnvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUe5bplNUUN3ME2xMlg6KM7:TR?= MVuyOFAxQTB4NB?=
BT474 NW\MS2tnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXGTIh4UUN3ME2wMlAxOzJ|INMxJFAvODByN{Wg{txO M3vXVlI{QDF4MkW0
SKBR3 M{P5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{K1e2lEPTB;MD6wNFc2KMLzIECuNFA2KM7:TR?= NYPhWWlvOjN6MU[yOVQ>
MDAMB453 NHf1fGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEOyUIRKSzVyPUGuOVkhyrFiMD6xO|kh|ryP MVSyN|gyPjJ3NB?=
KB NX\pbFZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHzNHJKSzVyPUSuNVMhyrFiMD60O{DPxE1? NGnwS48zOjR7MUmzOS=>
KBv200 NXXX[I1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M362[mlEPTB;Nj6wN{DDuSByLk[0JO69VQ>? NGnuSXEzOjR7MUmzOS=>
MCF-7 NFLQW2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\tU4hRUUN3ME2zMlMxKMLzIECuOFEh|ryP MWqyNlQ6OTl|NR?=
MCF-7/Adr Mlm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLBTWM2OD1iMj64PEDDuSByLkOwJO69VQ>? M1r4dVIzPDlzOUO1
MCF-7 NFn6dWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fabmlEPTB;Mz6wNkDDuSByLkO0JO69VQ>? M3XkNFIzPDlzOUO1
MCF-7/FLV1000 M2L2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XpU2lEPTB;Nz6wPUDDuSByLkexJO69VQ>? M1fwc|IzPDlzOUO1
HL60 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XHeGlEPTB;Mj6yOkDDuSByLkKzJO69VQ>? M3L3U|IzPDlzOUO1
HL60/Adr M4qyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;IU4J4UUN3ME2xMlQzKMLzIECuNVUh|ryP MnzXNlI1QTF7M{W=
HEK293/pcDNA3.1 NXPZVIw{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljnTWM2OD13LkK5JOKyKDBwNUOg{txO NFPUTIUzOjR7MUmzOS=>
HEK293/ABCB1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTZwOUGgxtEhOC55MDCg{txO M4XzWFIzPDlzOUO1
SKBR MnzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjyNE4xOS1zMECgcm0> M2K1elMuPyCm NE\JVI1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MoLGNlE1QDd4MEW=
L858R(EGFR) MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXTk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M4T1e|E4OzFzMECy
L858R/T790M(EGFR) M4DaPGNmdGxiVnnhZoltcXS7IFHzd4F6 Moq4[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MWGxO|MyOTByMh?=
G776insV_G/C MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4jTO4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M2nyclE4OzFzMECy
wild-type NYDkUGw5S2WubDDWbYFjcWyrdImgRZN{[Xl? M{LFUoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NHrqbG4yPzNzMUCwNi=>
A775insYVMA NUG3cY9FS2WubDDWbYFjcWyrdImgRZN{[Xl? MlXu[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NEXCOlQyPzNzMUCwNi=>
G776insV_G/L NXG5eWxxS2WubDDWbYFjcWyrdImgRZN{[Xl? MVrk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M1LHeVE4OzFzMECy
P780insGSP M{LuUWNmdGxiVnnhZoltcXS7IFHzd4F6 M{LpdoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NVPmTox2OTd|MUGwNFI>
NCI-H1781 M1jWS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjsdm5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NH\kO3AyPjhzOE[xPC=>
HCC827 M4W3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlywbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcpQhdWGwbnXy M1i1NlE3QDF6NkG4
H3255 M1LDT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTNdIlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NH;rXGQyPjhzOE[xPC=>
NCI-H1975 M1HjV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;RRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MmS2NVY5OTh4MUi=
A549 Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPpbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MXOxOlgyQDZzOB?=
3T3 Mn7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLiXWhjUUN3ME23NFAhyrFiN{igcm0> MVKxOVE4OzByOB?=
3T3/neu NH3pc2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTNiwsGgNE4yPCCwTR?= M4n5XFE2OTd|MEC4
SK-Br-3 Ml7kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWe0e2tGUUN3ME2yJOKyKDBwMUigcm0> M{HNNVE2OTd|MEC4
BT 474 NX;zclJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDMbpd6UUN3ME2yJOKyKDBwME[gcm0> MmnzNVUyPzNyMEi=
A431 M3TjeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRThzINMxJFkhdk1? M3zmelE2OTd|MEC4
MDA-MB-435 NFS3RVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnITWM2OD17NkCgxtEhOTZ3IH7N NXTXR2ZWOTVzN{OwNFg>
SW620 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3G2[mlEPTB;NkmwJOKyKDh2IH7N NHrEO3QyPTF5M{CwPC=>

... 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]
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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]
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  • 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]
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  • 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
Smiles CCOC1=C(NC(=O)\C=C\CN(C)C)C=C2C(=C1)N=CC(=C2NC3=CC=C(OCC4=NC=CC=C4)C(=C3)Cl)C#N

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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