PD173074

Licensed by Pfizer Catalog No.S1264

For research use only.

PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.

PD173074 Chemical Structure

CAS No. 219580-11-7

Selleck's PD173074 has been cited by 100 publications

Purity & Quality Control

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Biological Activity

Description PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.
Targets
FGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
~25 nM 100 nM-200 nM
In vitro

PD173074 is an ATP-competitive inhibitor of FGFR1 with Ki of ~40 nM. PD173074 is also an effective inhibitor of VEGFR2. Compared to FGFR1, PD173074 weakly inhibits the activities of Src, InsR, EGFR, PDGFR, MEK, and PKC with 1000-fold or greater IC50 values. PD173074 inhibits autophosphorylation of FGFR1 and VEGFR2 in a dose-dependent manner with IC50 of 1-5 nM and 100-200 nM, respectively. [1] PD173074 inhibits FGF-2 promotion of granule neuron survival in a dose-dependent manner with IC50 of 12 nM, exhibiting 1,000-fold greater potency than that of SU 5402. [2] PD173074 specifically inhibits FGF-2-mediated effects on proliferation, differentiation, and MAPK activation in oligodendrocyte (OL) lineage cells. [3] PD173074 is active against the WT receptor and FGFR3 mutations in multiple myeloma (MM) cell lines. PD173074 also potently inhibits autophosphorylation of FGFR3 in a dose-dependent manner with IC50 of ~5 nM. PD173074 treatment potently reduces viability of FGFR3-expressing KMS11 and KMS18 cells with IC50 of <20 nM. Inhibition of aFGF-stimulated MM cell growth by PD173074 is highly correlated with the expression of FGFR3. PD173074 treatment completely abolishes NIH 3T3 transformation mediated by Y373C FGFR3 but not by Ras V12, demonstrating that PD173074 specifically targets FGFR3-mediated cell transformation and lacks nonspecific cytotoxic effect. PD173074 also induces functional maturation of KMS11 and KMS18 cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 NYj2W4NoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;DU3RKSzVyPUCuNFEzOjVizszN M{O4UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
KG-1 NEPtZWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfSdoFKSzVyPUCuNFUyOjlizszN Mn;1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
MFM-223 MkTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfDTJhiUUN3ME2wMlIyPTd4IN88US=> MkXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
EoL-1-cell M1flTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Phc2lEPTB;MD6zNlk5PCEQvF2= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
ECC10 M1nkNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3juUGlEPTB;MD6zN|g6QCEQvF2= NFXjTHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
H-EMC-SS MmSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTFNFBiUUN3ME2wMlM1PzF3IN88US=> M3\PflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
AN3-CA M4XUcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELRUoZKSzVyPUCuOFAyOzNizszN NXr3[FdQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
HuO-3N1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjITWM2OD1yLkW0OlU{KM7:TR?= M3HQNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
RT-112 MnPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILl[plKSzVyPUCuOVQ4ODFizszN Ml\aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
NEC8 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDnTWM2OD1yLkW2Nlg6KM7:TR?= MmTGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
D-263MG NIiwZXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnizTWM2OD1yLkexNVU6KM7:TR?= MlrlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
SW962 NGXl[FhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTBwN{i5PFgh|ryP NWf6[o5pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
BV-173 M4H5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHS1OVNKSzVyPUCuPFQ3OjNizszN NG\YOmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
MFE-280 M1nrSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPyTGtpUUN3ME2wMlg2QDd{IN88US=> NGT4XW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
HuH-7 M174WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rQ[2lEPTB;MT6yOFQ3PCEQvF2= NY\ENVVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
RS4-11 NWC5cGNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTFwM{O4PFYh|ryP MmPmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
DMS-114 MomzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTFwM{[3N|ch|ryP MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
MSTO-211H M2PFWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLWOXA3UUN3ME2xMlQ4Ozd6IN88US=> NUO5TXl7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
DU-145 M{H3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\tNWlEPTB;MT61PFIyPyEQvF2= M2THfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
A172 MlO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PEXGlEPTB;MT63NFM2PSEQvF2= NFi1WJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
SBC-1 NGLrOG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHtd45KSzVyPUKuNFk1KM7:TR?= M3HCU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
H9 NF3QbmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DSOWlEPTB;Mj6xOFMxPiEQvF2= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
NCI-SNU-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TzT2lEPTB;Mj6xPFM6PCEQvF2= M3TEZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
NCI-H720 NX:1NFliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\TTpUzUUN3ME2yMlIyOjh|IN88US=> NXvi[FNkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
HCC2218 M2rPNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTBZ4ZKSzVyPUKuN|c6OzlizszN NYHn[JFORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
G-401 M3XjbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJwNEexPFkh|ryP M33TVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
MPP-89 NYfvU|lMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHO4SW1KSzVyPUKuOFg{PjRizszN NW\BUFdyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
697 NX;1SW95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4r1N2lEPTB;Mj62OVM{OSEQvF2= M4\pOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
KARPAS-45 NHj0TmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzLTWM2OD1{LkewO|Q4KM7:TR?= MkfCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
MG-63 MmnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\ISYduUUN3ME2yMlk1OjZ{IN88US=> NEPnUpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
NTERA-S-cl-D1 MoTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrxUldKSzVyPUOuNFM1PzJizszN MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
G-402 NVLsVpFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTNwMUK3Nlch|ryP NFq4[WU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
NKM-1 M3;RO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTuV5ppUUN3ME2zMlE{PTZ2IN88US=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
RH-18 NIS1VlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfJ[W1KSzVyPUOuNVk2QThizszN NFLRTW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
NCI-H1092 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEO5T45KSzVyPUOuNVk3QSEQvF2= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
RPMI-8226 NVTOeHFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln4TWM2OD1|LkKzOFQ4KM7:TR?= NY\XWVB[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
GAMG NUX4cJZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;KR3JCUUN3ME2zMlQ3PTd4IN88US=> M3iz[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
HH NF3LR3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTNwNEe2O|Yh|ryP NH\lVpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
RO82-W-1 MljOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELRUldKSzVyPUOuOFk5PTVizszN M4WyclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
CCRF-CEM NWm2R3NDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDsTWM2OD1|LkWwOFg5KM7:TR?= NXHs[YJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
NBsusSR MnLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTNwNkO5Olkh|ryP NVnVPHY4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
CHL-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLwcWhkUUN3ME2zMlY2Pzl7IN88US=> NE\OfIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
LK-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTNwNkexN|Mh|ryP NEPxTXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
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BT-37 MUTxTHRUKGG|c3H5 NYm3bGpleUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz MkHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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BT-12 NHrkUnpyUFSVIHHzd4F6 NXH0TYVbeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz NHS0RlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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OHS-50 NXix[IlweUiWUzDhd5NigQ>? MWjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MlvrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD MojZdWhVWyCjc4PhfS=> NE\OToZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
fibroblast cells NX;CNJZxeUiWUzDhd5NigQ>? NGmwNpRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiY3;ueJJwdCCKaDD3bYxlKHS7cHWg[oljem:kbHHzeEBk\Wyucx?= M17iO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 NXyye3l4eUiWUzDhd5NigQ>? MXXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? NWnh[IxVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Assay
Methods Test Index PMID
Western blot pFGFR2 / FGFR2 ; p-S6RP / p-PRAS40 / p-p105 NFKB / P105 NFKB / P50 NFKB / p-AMPK / p-CRK II / p-PDK1 24968263
Growth inhibition assay Cell viability 24968263
In vivo Administration of PD173074 at 1 mg/kg/day or 2 mg/ka/day in mice can effectively block angiogenesis induced by either FGF or VEGF in a dose-dependent manner with no apparent toxicity. [1] PD173074 inhibits in vivo growth of mutant FGFR3-transfected NIH 3T3 cells in nude mice. Inhibition of FGFR3 by PD173074 delays tumor growth and increases survival of mice in a KMS11 xenograft myeloma model. [4] In the H-510 xenograft, oral aministration of PD173074 blocks tumor growth similar to that seen with single-agent cisplatin administration, increasing median survival compared with control sham-treated animals. In H-69 xenografts, PD173074 induces complete responses lasting >6 months in 50% of mice. These effects are correlated with increased apoptosis in excised tumors, but not a consequence of disrupted tumor vasculature. [5]

Protocol (from reference)

Kinase Assay:[1]
  • In vitro kinase inhibition assays:

    Assays using the full-length FGFR-1 kinase are performed in a total volume of 100 μL containing 25 mM HEPES buffer (pH 7.4), 150 mM NaCl, 10 mM MnCl2, 0.2 mM sodium orthovanadate, 750 μg/mL concentration of a random copolymer of glutamic acid and tyrosine (4:1), various concentrations of PD173074 and 60 to 75 ng of enzyme. The reaction is initiated by the addition of [γ-32P]ATP (5 μM ATP containing 0.4 μCi of [γ-32P]ATP per incubation), and samples are incubated at 25°C for 10 minutes. The reaction is terminated by the addition of 30% trichloroacetic acid and the precipitation of material onto glass-fiber filter mats. Filters are washed three times with 15% trichloroacetic acid, and the incorporation of [32P] into the glutamate tyrosine polymer substrate is determined by counting the radioactivity retained on the filters in a Wallac 1250 betaplate reader. Nonspecific activity is defined as radioactivity retained on the filters following incubation of samples without enzyme. Specific activity is determined as total activity (enzyme plus buffer) minus nonspecific activity. The concentration of PD173074 that inhibits FGFR-1 enzymatic activity by 50% (IC50) is determined graphically.

Cell Research:[4]
  • Cell lines: KMS11 and KMS18
  • Concentrations: Dissolved in DMSO, final concentrations ~100 nM
  • Incubation Time: 48 hours
  • Method: Cells are incubated with increasing concentrations of PD173074 in the presence of aFGF/heparin for 48 hours. The percentage of viable cells is determined by MTT.
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: Swiss Webster mice with induced corneal angiogenesis
  • Dosages: ~2 mg/kg/day
  • Administration: Administered intraperitoneally
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(190.95 mM)
Ethanol 100 mg/mL
(190.95 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.

15mg/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 523.67
Formula

C28H41N7O3

CAS No. 219580-11-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C

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

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:
What is the half-life of PD173074(S1264) in vivo?

Answer:
According to literature research, PD173074 is given twice daily because it has a short half-life in vivo, please refer to the following link for detailed pharmacokinetic information (Supplementary Figure 8B): http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3990281/#!po=50.0000.

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