Infigratinib (BGJ398)

Catalog No.S2183 Synonyms: NVP-BGJ398

For research use only.

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.

Infigratinib (BGJ398) Chemical Structure

CAS No. 872511-34-7

Selleck's Infigratinib (BGJ398) has been cited by 188 publications

Purity & Quality Control

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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 NYD5SFdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTvPVQ{OS1{NUCwJI5O MUm0PEBp NVvudYV5UUN3ME2gNlM2QeLCiX7t NY\PdHcyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2PFg4PDNpPkK1Olg5PzR|PD;hQi=>
HCC NFm1VXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{i1U|EuOjVyMDDuUS=> M{nVeVQ5KGh? M3rVbWlEPTB;MUGyOQKBkW6v MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ6OEe0N{c,OjV4OEi3OFM9N2F-
HCT116 M375dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzZZXM1QCCq MYrJR|UxRTNizszN NF65O|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwN|U{QCd-MkS1NFM2Ozh:L3G+
HKH2 M3\Wemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWS0PEBp MoXQTWM2OD12IN88US=> MnvoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3MEO1N|goRjJ2NUCzOVM5RC:jPh?=
RKO NF3tVZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[0PEBp NUDxNnFEUUN3ME2xMlIh|ryP NXS0R45iRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1NFM2OzhpPkK0OVA{PTN6PD;hQi=>
LS174T MnTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DLZlQ5KGh? MWTJR|UxRTRizszN NHTSSIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwN|U{QCd-MkS1NFM2Ozh:L3G+
HCD9 NUWx[XFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3wOo55OC53LUWg{txO M4XrO|Q5Nzd{IHi= M2DzdmROW09? MmLF[IVkemWjc3XzJINmdGxidnnhZoltcXS7 M{CwUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUO1PFE3Lz5{NEGzOVgyPjxxYU6=
HCT116 NUHQbYRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqwMlUuPSEQvF2= MX60PE84OiCq NXLV[XBiTE2VTx?= MX3k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? MoTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzM{W4NVYoRjJ2MUO1PFE3RC:jPh?=
SNU-C1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHqdVgxNjVvNTFOwG0> MlL0OFgwPzJiaB?= NHf0TZRFVVOR NFW3OmNvdyCnZn\lZ5Q> NEjmSYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGzOVgyPid-MkSxN|U5OTZ:L3G+
MFE280 NELlNGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTJwNkOgxtEhOC56MjFOwG0> MmHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEO4NFUoRjJ|NESzPFA2RC:jPh?=
AN3CA MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jV[WlEPTB;MT6wNEDDuSByLkKwJO69VQ>? NF;udmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0N|gxPSd-MkO0OFM5ODV:L3G+
HEC155 NWPofGM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEGyN|dKSzVyPUSuO|QhyrFiMT6wPUDPxE1? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR2M{iwOUc,OjN2NEO4NFU9N2F-
MFE296 Mlq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJwOE[gxtEhOC5{MDFOwG0> M1zXR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NESzPFA2Lz5{M{S0N|gxPTxxYU6=
SPAC1S NGfYPJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\TcGlEPTB;Mz6xPUDDuSByLkmzJO69VQ>? NEfVN489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0N|gxPSd-MkO0OFM5ODV:L3G+
RL952 M2qxemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXpOGdKSzVyPUOuOFEhyrFiMD6yN{DPxE1? NWPyN3R5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OFM5ODVpPkKzOFQ{QDB3PD;hQi=>
EN1 NEmwTIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVOyb3V[UUN3ME20Mlc2KMLzIECuOlIh|ryP NYK0fVF[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OFM5ODVpPkKzOFQ{QDB3PD;hQi=>
SNGII M3PuWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXJ[lVOUUN3ME20MlI6KMLzIECuOVgh|ryP NUK3[G4yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OFM5ODVpPkKzOFQ{QDB3PD;hQi=>
ISHIKAWA MmO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXmTWM2OD13LkS4JOKyKDBwMEOg{txO MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR2M{iwOUc,OjN2NEO4NFU9N2F-
HEC1A NV\SSodbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTvRXFPUUN3ME2xNE4xOCEEsTCxMlAxKM7:TR?= MnTiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEO4NFUoRjJ|NESzPFA2RC:jPh?=
KLE MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTNwMEOgxtEhOC5zMTFOwG0> M37F[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NESzPFA2Lz5{M{S0N|gxPTxxYU6=
SNGM NFnmSm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTVwMECgxtEhOC52MTFOwG0> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR2M{iwOUc,OjN2NEO4NFU9N2F-
USPC2 NGnzZ5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTdwMECgxtEhOC5{MTFOwG0> NIXRV2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0N|gxPSd-MkO0OFM5ODV:L3G+
EN NWPlSoFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInnfXNKSzVyPU[uNFMhyrFiMD6zNUDPxE1? MmnnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEO4NFUoRjJ|NESzPFA2RC:jPh?=
MFE319 M3vPdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfWb5BKSzVyPUWuN|chyrFiMD6wN{DPxE1? NF;6bJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0N|gxPSd-MkO0OFM5ODV:L3G+
EFE184 Ml25S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXmN3RIUUN3ME24MlA1KMLzIECuOlkh|ryP M4nGZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NESzPFA2Lz5{M{S0N|gxPTxxYU6=
ECC1 NX25c2FIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHLTWM2OD14Lke0JOKyKDBwNUmg{txO M4jOW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NESzPFA2Lz5{M{S0N|gxPTxxYU6=
HEC1B Mk\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTZwNEWgxtEhOC54NzFOwG0> NWTLR3NRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OFM5ODVpPkKzOFQ{QDB3PD;hQi=>
USPC1 NGDYXHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3sTWM2OD13Lke1JOKyKDBwNUCg{txO NEnXUpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0N|gxPSd-MkO0OFM5ODV:L3G+
SPAC1L NIPsWldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{H5c2lEPTB;ND65NkDDuSByLkWwJO69VQ>? MoDOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEO4NFUoRjJ|NESzPFA2RC:jPh?=
HCC827 MkfFSpVv[3Srb36gZZN{[Xl? MWrEbZNxdGGlZX3lcpQhd2ZiW{PIYU1kgWOub4DhcYlv\SCocn;tJHNOVyCYNEC0UUBufXSjboSgbY4h\2WoaYTpcoljKHKnc3nzeIFvfCCqdX3hckBJS0N6MkegZ4VtdHNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiS3mgQUAxNjB2NkWg{txONg>? NHjnd|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe4O|E2Pid-Mki3PFcyPTZ:L3G+
SJ-GBM2 M3zKcJFJXFNiYYPzZZk> M4\1VZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz M3;iVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 MojBdWhVWyCjc4PhfS=> NXnYNlIxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> NIjqRWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
sf9 Mkj6SpVv[3Srb36gZZN{[Xl? MmrzOlAhdWmwcx?= NETheI9KdmirYnn0bY9vKG:oIH7vck1xcG:|cHjvdplt[XSnZDDOMZRmem2rbnHsJGhqezZvdHHn[4VlKE[JRmK0JGM2PTKDIH31eIFvfCBqR{S0NkB1dyCHN{WzJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiC|ZkmgZ4VtdHNidYPpcochPS2IbIXvMWFpgC2NS1vLSWVKYU[IRletUmgzKGG|IIP1ZpN1emG2ZTDh[pRmeiB4MDDtbY5{KGK7IH3pZ5Jw\my3aXTpZ{Bud2KrbHn0fUB{cGmodDDhd5NigSxiSVO1NEA:KDBwMECwPFIh|ryPLh?= Mn\MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg2OjZ6OD:nQmNpTU2ETEyvZV4>
sf9 MYjGeY5kfGmxbjDhd5NigQ>? MmLIOlAhdWmwcx?= NGm2PHRKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDuc44ueGixc4Doc5J6dGG2ZXSgUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCIR1\SOEApTzR2MjD0c{BGPzV|IILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckB{\jliY3XscJMhfXOrbnegOU1HdHWxLVHofE1MU0uNRVXJXWZHTkdvTliyJIF{KHO3YoP0doF1\SCjZoTldkA3OCCvaX7zJIJ6KG2rY4Lv[ox2cWSrYzDtc4JqdGm2eTDzbIlnfCCjc4PhfUwhUUN3MDC9JFAvODZ{IN88UU4> NHfOdZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDV{Nki4M{c,S2iHTVLMQE9iRg>?
sf9 MkCwSpVv[3Srb36gZZN{[Xl? M{LOO|YxKG2rboO= MV3Jcohq[mm2aX;uJI9nKG6xbj3wbI9{eGixconsZZRm\CCQLYTldo1qdmGuIFjpd|YufGGpZ3XkJGZITlJ2IFO0O|dCKG23dHHueEApTzR2MjD0c{BGPzV|IILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckB{\jliY3XscJMhfXOrbnegOU1HdHWxLVHofE1MU0uNRVXJXWZHTkdvTliyJIF{KHO3YoP0doF1\SCjZoTldkA3OCCvaX7zJIJ6KG2rY4Lv[ox2cWSrYzDtc4JqdGm2eTDzbIlnfCCjc4PhfUwhUUN3MDC9JFAvODZ2IN88UU4> MnLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg2OjZ6OD:nQmNpTU2ETEyvZV4>
Assay
Methods Test Index PMID
Western blot pFGFR1 / FGFR1 / pFRS2 / FRS2 / MEK / ERK ; p-YAP (S127) / YAP ; Mcl-1 ; Cyclin D1 / Cyclin A / Cyclin B / γ-H2AX / Cleaved caspase-9 / PARP ; Snail / Slug / ZEB1 ; p-FRS2 / FRS2 / p-AKT / AKT / p-ERK / ERK 28255027 26826125 30326563 29654068
Immunofluorescence YAP 26826125
Growth inhibition assay Cell viability ; IC50 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 (from reference)

Kinase Assay: [1]
  • 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]
  • 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.
Animal Research:[1]
  • Animal Models: Athymic nude-nu mice bearing parental RT112 cell line
  • Dosages: 10 mg/kg/qd and 30 mg/kg/qd
  • Administration: Oral administration

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 560.48
Formula

C26H31Cl2N7O3

CAS No. 872511-34-7
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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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