Infigratinib (BGJ398)

For research use only.

Catalog No.S2183 Synonyms: NVP-BGJ398

165 publications

Infigratinib (BGJ398) Chemical Structure

CAS No. 872511-34-7

Infigratinib (BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.

Selleck's Infigratinib (BGJ398) has been cited by 165 publications

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Biological Activity

Description Infigratinib (BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.
Targets
FGFR1 [1]
(Cell-free assay)
FGFR3 [1]
(Cell-free assay)
FGFR2 [1]
(Cell-free assay)
FGFR3 (K650E) [1]
(Cell-free assay)
FGFR4 [1]
(Cell-free assay)
0.9 nM 1.0 nM 1.4 nM 4.9 nM 60 nM
In vitro

BGJ398 also prevents VEGFR2 with low potency. The IC50 of BGJ398 for inhibiting VEGFR2 is 0.18 μM. BGJ398 suppresses other kinases including ABL, FYN, KIT, LCK, LYN and YES with IC50 of 2.3 μM, 1.9 μM, 0.75 μM, 2.5 μM, 0.3 μM and 1.1 μM, respectively. At the cellular level, BGJ398 inhibits the proliferation of the FGFR1-, FGFR2-Q, and FGFR3-dependent BaF3 cells with IC50 of 2.9 μM, 2.0 μM and 2 μM, respectively. BGJ398 interferes with autophosphorylation on specific tyrosine residues including FGFR-WT, FGFR2-WT, FGFR3-K650E, FGFR3-S249C and FGFR4-WT with IC50 of 4.6 nM, 4.9 nM, 5 nM, 5 nM and 168 nM, respectively. BGJ398 suppresses proliferation of the cancer cells with wild-type (WT) FGFR3 overexpression such as RT112, RT4, SW780 and JMSU1 with IC50 of 5 nM, 30 nM, 32 nM and 15 nM, respectively. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC MlHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXE[VJnOS1{NUCwJI5O NWDNOVJHPDhiaB?= MoW1TWM2OD1iMkO1PgKBkW6v NEPzUpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[4PFc1Oyd-MkW2PFg4PDN:L3G+
HCC NGXCS|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXexMVI2ODBibl2= NGTobI01QCCq NHftTVNKSzVyPUGxNlTjiImwbR?= MmS1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4OEi3OFMoRjJ3Nki4O|Q{RC:jPh?=
HCT116 MnSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3KzUVQ5KGh? NHrnOI1KSzVyPUOg{txO NXzPTZdIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1NFM2OzhpPkK0OVA{PTN6PD;hQi=>
HKH2 NVnoNpdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3iOFghcA>? NVHYdJRmUUN3ME20JO69VQ>? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVyM{WzPEc,OjR3MEO1N|g9N2F-
RKO NHjISIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LLRlQ5KGh? NGPyVGlKSzVyPUGuNkDPxE1? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVyM{WzPEc,OjR3MEO1N|g9N2F-
LS174T NGn5UmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:0PEBp MXvJR|UxRTRizszN Mn7zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3MEO1N|goRjJ2NUCzOVM5RC:jPh?=
HCD9 M3nKbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLxNE42NTVizszN M1XTZlQ5Nzd{IHi= M2fTe2ROW09? MlvU[IVkemWjc3XzJINmdGxidnnhZoltcXS7 M3f4WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUO1PFE3Lz5{NEGzOVgyPjxxYU6=
HCT116 Ml3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXyydYhGOC53LUWg{txO NXq3OWV3PDhxN{KgbC=> M3rV[mROW09? MkTV[IVkemWjc3XzJINmdGxidnnhZoltcXS7 NYKySpM6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxN|U5OTZpPkK0NVM2QDF4PD;hQi=>
SNU-C1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPhUWIxNjVvNTFOwG0> MkDNOFgwPzJiaB?= MkLwSG1UVw>? NIPoboZvdyCnZn\lZ5Q> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF|NUixOkc,OjRzM{W4NVY9N2F-
MFE280 NEjK[4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HzPWlEPTB;Mj62N{DDuSByLkiyJO69VQ>? M4XDN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NESzPFA2Lz5{M{S0N|gxPTxxYU6=
AN3CA NILKWWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTFwMECgxtEhOC5{MDFOwG0> Mon5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEO4NFUoRjJ|NESzPFA2RC:jPh?=
HEC155 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGn4VHlKSzVyPUSuO|QhyrFiMT6wPUDPxE1? Mk\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEO4NFUoRjJ|NESzPFA2RC:jPh?=
MFE296 MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLzSWZKSzVyPUKuPFYhyrFiMD6yNEDPxE1? NGezNms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0N|gxPSd-MkO0OFM5ODV:L3G+
SPAC1S NFfXWmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX62[ndYUUN3ME2zMlE6KMLzIECuPVMh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR2M{iwOUc,OjN2NEO4NFU9N2F-
RL952 Mo\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGH3cGNKSzVyPUOuOFEhyrFiMD6yN{DPxE1? M3e2SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NESzPFA2Lz5{M{S0N|gxPTxxYU6=
EN1 M1vSTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTRwN{WgxtEhOC54MjFOwG0> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR2M{iwOUc,OjN2NEO4NFU9N2F-
SNGII MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjLPVdKSzVyPUSuNlkhyrFiMD61PEDPxE1? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR2M{iwOUc,OjN2NEO4NFU9N2F-
ISHIKAWA M13Pc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEG4UmFKSzVyPUWuOFghyrFiMD6wN{DPxE1? NUP4UG82RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OFM5ODVpPkKzOFQ{QDB3PD;hQi=>
HEC1A MlXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mly5TWM2OD1zMD6wNEDDuSBzLkCwJO69VQ>? NFK3bXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0N|gxPSd-MkO0OFM5ODV:L3G+
KLE Mk\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HIWGlEPTB;Mz6wN{DDuSByLkGxJO69VQ>? NHm0NVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0N|gxPSd-MkO0OFM5ODV:L3G+
SNGM NUPOe21TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorJTWM2OD13LkCwJOKyKDBwNEGg{txO NX3Kdpo3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OFM5ODVpPkKzOFQ{QDB3PD;hQi=>
USPC2 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nOfGlEPTB;Nz6wNEDDuSByLkKxJO69VQ>? MlyyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEO4NFUoRjJ|NESzPFA2RC:jPh?=
EN NEeyW5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fqcGlEPTB;Nj6wN{DDuSByLkOxJO69VQ>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR2M{iwOUc,OjN2NEO4NFU9N2F-
MFE319 NWLNcGtYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{ezemlEPTB;NT6zO{DDuSByLkCzJO69VQ>? MmrUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEO4NFUoRjJ|NESzPFA2RC:jPh?=
EFE184 NYK5NHpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRThwMESgxtEhOC54OTFOwG0> M2n6U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NESzPFA2Lz5{M{S0N|gxPTxxYU6=
ECC1 M3vWSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mne4TWM2OD14Lke0JOKyKDBwNUmg{txO Mn;0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEO4NFUoRjJ|NESzPFA2RC:jPh?=
HEC1B MkPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zrb2lEPTB;Nj60OUDDuSByLk[3JO69VQ>? NETTOXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0N|gxPSd-MkO0OFM5ODV:L3G+
USPC1 M1jPWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fQRmlEPTB;NT63OUDDuSByLkWwJO69VQ>? NYTEelVmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OFM5ODVpPkKzOFQ{QDB3PD;hQi=>
SPAC1L NX7He5J{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTRwOUKgxtEhOC53MDFOwG0> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR2M{iwOUc,OjN2NEO4NFU9N2F-
HCC827 M4LQXWZ2dmO2aX;uJIF{e2G7 Mnr5SIl{eGyjY3Xt[Y51KG:oIGuzTH0u[3mlbH;wZY1qdmViZoLvcUBUVU9iVkSwOG0hdXW2YX70JIlvKGenZnn0bY5q[iC{ZYPpd5RidnRiaIXtZY4hUEOFOEK3JINmdGy|IHL5JJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFvpJF0hOC5yNE[1JO69VS5? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd6N{G1Okc,Ojh5OEexOVY9N2F-
SJ-GBM2 NHf5R5dyUFSVIHHzd4F6 NHjHfJRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 MmrDdWhVWyCjc4PhfS=> MXTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NH\EN489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
sf9 M4HVR2Z2dmO2aX;uJIF{e2G7 MYO2NEBucW6| NGrHUYlKdmirYnn0bY9vKG:oIH7vck1xcG:|cHjvdplt[XSnZDDOMZRmem2rbnHsJGhqezZvdHHn[4VlKE[JRmK0JGM2PTKDIH31eIFvfCBqR{S0NkB1dyCHN{WzJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiC|ZkmgZ4VtdHNidYPpcochPS2IbIXvMWFpgC2NS1vLSWVKYU[IRletUmgzKGG|IIP1ZpN1emG2ZTDh[pRmeiB4MDDtbY5{KGK7IH3pZ5Jw\my3aXTpZ{Bud2KrbHn0fUB{cGmodDDhd5NigSxiSVO1NEA:KDBwMECwPFIh|ryPLh?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFUzPjh6Lze+R4hGVUKOPD;hQi=>
sf9 MojCSpVv[3Srb36gZZN{[Xl? NHzUTXA3OCCvaX7z NH\WWo1KdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDuc44ueGixc4Doc5J6dGG2ZXSgUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCIR1\SOEApTzR2MjD0c{BGPzV|IILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckB{\jliY3XscJMhfXOrbnegOU1HdHWxLVHofE1MU0uNRVXJXWZHTkdvTliyJIF{KHO3YoP0doF1\SCjZoTldkA3OCCvaX7zJIJ6KG2rY4Lv[ox2cWSrYzDtc4JqdGm2eTDzbIlnfCCjc4PhfUwhUUN3MDC9JFAvODZ{IN88UU4> NWnjPGVpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh3Mk[4PE8oRkOqRV3CUFww[T5?
sf9 NILwOGdHfW6ldHnvckBie3OjeR?= NFTLZY43OCCvaX7z MYnJcohq[mm2aX;uJI9nKG6xbj3wbI9{eGixconsZZRm\CCQLYTldo1qdmGuIFjpd|YufGGpZ3XkJGZITlJ2IFO0O|dCKG23dHHueEApTzR2MjD0c{BGPzV|IILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckB{\jliY3XscJMhfXOrbnegOU1HdHWxLVHofE1MU0uNRVXJXWZHTkdvTliyJIF{KHO3YoP0doF1\SCjZoTldkA3OCCvaX7zJIJ6KG2rY4Lv[ox2cWSrYzDtc4JqdGm2eTDzbIlnfCCjc4PhfUwhUUN3MDC9JFAvODZ2IN88UU4> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFUzPjh6Lze+R4hGVUKOPD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pFGFR1 / FGFR1 / pFRS2 / FRS2 / MEK / ERK; 

PubMed: 28255027     


Immunoblot demonstrates the expression of total/pFGFRs and total/pFRS2 in DMSO and BGJ398 in treated cell lines A. DMS114. B. RT112. Lysates were prepared from cells exposed to BGJ398 (at the indicated concentrations) for 24h and immunoblots performed with the respective antibodies. Representative data are shown from three experimental replicates. Bar graphs display densitometric analysis of protein bands using GAPDH as control. BGJ398 treatment results in decreased levels of pFGFR1/pFGFR3 and pFRS2/total FRS2, respectively.

p-YAP (S127) / YAP; 

PubMed: 26826125     


Immunoblot analysis of serine 127-phosphorylated YAP (p-YAPS127) and total YAP in KMCH and KMBC cells treated with vehicle (Veh) or BGJ398 (10 μm) for 24 h. β-Actin was used as a loading control.

Mcl-1; 

PubMed: 26826125     


Immunoblot analysis (E) of Mcl-1 in KMCH and KMBC cells treated with vehicle or BGJ398 (10 μm) at several time points. β-Actin was used as a loading control.

Cyclin D1 / Cyclin A / Cyclin B / γ-H2AX / Cleaved caspase-9 / PARP ; 

PubMed: 30326563     


Cells were treated with indicated concentration of PTX and BGJ398 for 24 h. Expression of cyclin D1, cyclin A, cyclin B, γ-H2AX, caspase-9, PARP, and β-actin (loading control) was analyzed by Western blotting.

Snail / Slug / ZEB1; 

PubMed: 30326563     


PTX and BGJ398 combination treatment synergistically decreases the protein levels of EMT inducers Snail, Slug, and ZEB1.

p-FRS2 / FRS2 / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 29654068     


Protein lysates from NCI-H2077 cells after treatment with DMSO or BGJ398 1 μM probed at different time points for key members of the canonical FGFR signaling pathway.

28255027 26826125 30326563 29654068
Immunofluorescence
YAP; 

PubMed: 26826125     


Immunofluorescence images (top panel) and percentage of YAP-positive nuclei (bottom panel) in KMCH and KMBC cells 24 h of treatment with 10 μmBGJ398. Mean ± S.E. are depicted for n = 3. **, p < 0.01. Scale bars: 50 μm.

26826125
Growth inhibition assay
Cell viability; 

PubMed: 28255027     


Resistance was induced by chronic exposure of DMS114, and RT112 cell lines to BGJ398. Control cells were treated with DMSO. Panel shows viability curves performed with CellTiter-Glo assay. Control and resistant cells were treated with BGJ398 at different concentrations as indicated, and viable cells were measured after 72h. The percentage of viable cells is shown relative to DMSO vehicle treated controls (mean ± SD). Assays were performed in quadruplicates (three experimental replicates).

IC50; 

PubMed: 30326563     


T24, J82, RT4, and UMUC-14 cells were treated with 0, 0.1, 1, and 10 μM BJG398 for 3 days. IC50 values were calculated using CalcuSyn (BioSoft, Ferguson, MO, USA). Data represent mean ± standard deviation of five replicates.

28255027 30326563
In vivo In this orthotopic xenograft bladder cancer model, BGJ398 induces tumor growth inhibition and stasis after oral administration for 12 consecutive days at the doses of 10 and 30 mg/kg, respectively. Interestingly, the animals that received BGJ398 exhibits either no body weight loss (10 mg/kg) or 10% body weight gain (30 mg/kg), a further indication of efficacy. RT112 tumor-bearing and female Rowett rats receive a single oral administration of the monophosphate salt of BGJ398 at the doses of 4.25 and 8.51 mg/kg. BGJ398 significantly decreases the levels of pFRS2 and pMAPK in a dose-dependent manner. BGJ398 inhibits significantly bFGF-stimulated angiogenesis in a dose-dependent manner. However, BGJ398 does not impair VEGF-induced blood vessel formation. [1]

Protocol

Kinase Assay: [1]
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Radiometric kinase assay:

The enzymatic kinase activity is assessed by measuring the phosphorylation of a synthetic substrate by the purified GST-fusion FGFR3-K650E kinase domain, in the presence of radiolabeled ATP. Enzyme activities are measured by mixing 10 μL of a 3-fold concentrated BGJ398 solution or control with 10 μL of the corresponding substrate mixture (peptidic substrate, ATP and [γ33P]ATP). The reactions are initiated by addition of 10 μL of a 3-fold concentrated solution of the enzyme in assay buffer. The final concentrations of the assay components are as following: 10 ng of GST-FGFR3-K650E, 20 mM Tris-HCl, pH 7.5, 3 mM MnCl2, 3 mM MgCl2, 1 mM DTT, 250 μg/mL PEG 20000, 2 μg/mL poly(EY) 4:1, 1% DMSO and 0.5 μM ATP (γ-[33P]-ATP 0.1 μCi). The assay is carried out according to the filter binding (FB) method in 96-well plates at room temperature for 10 minutes in a final volume of 30 μL including BGJ398. The enzymatic reactions are stopped by the addition of 20 μL of 125 mM EDTA, and the incorporation of 33P into the polypeptidic substrates is quantified as following: 30 μL of the stopped reaction mixture are transferred onto Immobilon-PVDF membranes previously soaked for 5 minutes with methanol, rinsed with water, soaked for 5 min with 0.5% H3PO4, and mounted on vacuum manifold with disconnected vacuum source. After spotting, vacuum is connected, and each well rinsed with 0.5% H3PO4 (200 μL). Free membranes are removed and ished four times on a shaker with 1% H3PO4 and once with ethanol. Membranes are dried and overlaid with addition of 10 μL/well of a scintillation fluid. The plates are eventually sealed and counted in a microplate scintillation counter. IC50 values are calculated by linear regression analysis of the percentage inhibition of the BGJ398.
Cell Research:[1]
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  • Cell lines: Murine BaF3 cell lines
  • Concentrations: 0 μM-0.1 μM
  • Incubation Time: 48 hours
  • Method: Murine BaF3 cell lines, whose proliferation and survival has been rendered IL-3-independent by stable transduction with tyrosine kinases activated either by mutation or fusion with a dimerizing partner, are cultured in RPMI-1640 media supplemented with 10% FBS, 4.5 g/L glucose, 1.5 g/L sodium bicarbonate, and Pen/Strep. Cells are passaged twice weekly. BGJ398-mediated inhibition of BaF3 cell proliferation and viability is assessed using a Luciferase bioluminescent assay. Exponentially growing BaF3 or BaF3 Tel-TK cells are seeded into 384-well plates (4250 cells/well) at 50 μL/well using a μFill liquid dispenser in fresh medium. BGJ398 is serially diluted in DMSO and arrayed in a polypropylene 384-well plate. Then 50 nL of BGJ398 are transferred into the plates containing the cells by using the pintool transfer device, and the plates incubated at 37 °C (5% CO2) for 48 hours. Then 25 μL of Bright-Glo are added, and luminescence is quantified using an Analyst-GT. Custom curve-fitting software is used to produce a logistic fit of percent cell viability as a function of the logarithm of inhibitor concentration. The IC50 value is determined as the concentration of BGJ398 needed to reduce cell viability to 50% of a DMSO control.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Athymic nude-nu mice bearing parental RT112 cell line
  • Dosages: 10 mg/kg/qd and 30 mg/kg/qd
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 1 mg/mL warmed (1.78 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1%CMC-Na
For best results, use promptly after mixing.
30mg/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 560.48
Formula

C26H31Cl2N7O3

CAS No. 872511-34-7
Storage powder
in solvent
Synonyms NVP-BGJ398
Smiles CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

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 SDS / 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
NCT03510455 Terminated Drug: BGJ398 Tumor-Induced Osteomalacia|Oncogenic Osteomalacia National Institute of Dental and Craniofacial Research (NIDCR)|National Institutes of Health Clinical Center (CC) February 27 2019 Phase 2
NCT02312804 Withdrawn Drug: BGJ398|Drug: Carboplatin|Drug: Paclitaxel Cancer of Cervix|Tumors The University of Texas Health Science Center at San Antonio January 2015 Phase 1
NCT02160041 Terminated Drug: BGJ398 Solid Tumor|Hematologic Malignancies Novartis Pharmaceuticals|Novartis July 24 2014 Phase 2
NCT01928459 Completed Drug: BGJ398|Drug: BYL719 Advanced Solid Tumors|Metastatic Solid Tumors Novartis Pharmaceuticals|Novartis October 2013 Phase 1
NCT01004224 Completed Drug: BGJ398 Advanced Solid Tumors With Alterations of FGFR1 2 and or 3|Squamous Lung Cancer With FGFR1 Amplification|Bladder Cancer With FGFR3 Mutation or Fusion|Advanced Solid Tumors With FGFR1 Amplication|Advanced Solid Tumors With FGFR2 Amplication|Advanced Solid Tumors With FGFR3 Mutation Novartis Pharmaceuticals|Novartis December 11 2009 Phase 1

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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Frequently Asked Questions

  • Question 1:

    If you have any suggestions about the formulation of this compound for a direct oral gavage administration?

  • Answer:

    BGJ398 (S2183) can be dissolved in 30% PEG400/0.5% Tween80/5% Propylene glycol at 30 mg/ml as a suspension.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID