219580-11-7
1-tert-butyl-3-[2-{[4-(diethylamino)butyl]amino}-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea
CAS: 219580-11-7
Molecular Formula: C28H41N7O3
219580-11-7 - Names and Identifiers
| Name | 1-tert-butyl-3-[2-{[4-(diethylamino)butyl]amino}-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea |
| Synonyms | CS-458 PD173074 PD-173074 PD 173074 1-tert-butyl-3-[2-{[4-(diethylamino)butyl]amino}-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea 1-(tert-butyl)-3-(2-((4-(diethylaMino)butyl)aMino)-6-(3,5-diMethoxyphenyl)pyrido[2,3-d]pyriMidin-7-yl)urea N-[2-[[4-(diethylaMino)butyl]aMino]-6-(3,5-diMethoxyphenyl)pyrido[2,3-d ]pyriMidin-7-yl]-N'-(1,1-diMethylethyl)- n-[2-[[4-(diethylamino)butyl]amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-n'-(1,1-dimethylethyl)urea Urea, N-[2-[[4-(diethylamino)butyl]amino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)- |
| CAS | 219580-11-7 |
| InChI | InChI=1/C28H41N7O3/c1-8-35(9-2)13-11-10-12-29-26-30-18-20-16-23(19-14-21(37-6)17-22(15-19)38-7)25(31-24(20)32-26)33-27(36)34-28(3,4)5/h14-18H,8-13H2,1-7H3,(H3,29,30,31,32,33,34,36) |
219580-11-7 - Physico-chemical Properties
| Molecular Formula | C28H41N7O3 |
| Molar Mass | 523.67 |
| Density | 1.163 |
| Melting Point | 82-85°C |
| Solubility | Soluble in DMSO (21 mg/ml), ethanol (100 mM), water (partly miscible), methanol, and ch |
| Appearance | Yellow solid |
| Color | yellow |
| pKa | 10.12±0.43(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Refractive Index | 1.598 |
| MDL | MFCD08705327 |
| Use | Potent inhibitor of FGF and VEGF (Flt/Flk) receptors. |
| In vitro study | PD173074 is an ATP-competitive inhibitor of FGFR1 with a K I of approximately 40 nM. PD173074 is also a potent inhibitor of VEGFR2. Compared to FGFR1,PD173074 weakly inhibited the activities of Src,INSR,EGFR,PDGFR,MEK and PKC, and the IC 50 value was more than 1000-fold greater. PD173074 dose-dependently inhibited the autophosphorylation of FGFR1 and VEGFR2 with IC50 values of 1-5 nM and 100-200 nM, respectively. PD173074 inhibited FGF-2-promoted survival of granular neurons in a dose-dependent manner with an IC50 of 12 nM and an activity of more than 1,000-fold that of SU 5402. D173074 specifically inhibits FGF-2-mediated cell proliferation, differentiation and MAPK activation of oligodendrocyte (OL) lineage cells. In multiple myeloma (MM) cell lines, PD173074 is active on wild receptor and FGFR3 mutations. PD173074 also potently inhibited FGFR3 autophosphorylation in a dose-dependent manner with an IC50 of approximately 5 nM. PD173074 strongly reduced the viability of fgfr3-expressing KMS11 and KMS18 cells with an IC50 of less than 20 nM. Inhibition of aFGF-stimulated MM cell growth by PD173074 is highly correlated with the expression of fgfr3. PD173074 completely inhibited NIH 3T3 conversion mediated by Y373C FGFR3 but not Ras, suggesting that PD173074 is specifically directed against FGFR3 gene-mediated cellular transformation and lacks non-specific cytotoxic effects. PD173074 also induced functional maturation of KMS11 and KMS18 cells. |
| In vivo study | PD173074 administered to mice at 1 mg/kg/day or 2 mg/kg/day effectively prevented angiogenesis induced by FGF or VEGF in a dose-dependent manner, there was no significant toxicity. PD173074 inhibits the growth of FGFR3 mutant-transfected NIH 3T3 cells in nude mice. In the KMS11 xenograft tumor model, PD173074 inhibition of FGFR3 resulted in tumor growth retardation and increased survival in mice. In H-510 xenografts, PD173074 blocked tumor growth similarly to cisplatin, increasing median survival compared to control sham-treated animals. The induction of PD173074 in 50% mice was longer than 6 months in H-69 xenografts. These effects are associated with increased apoptosis in resected tumors, rather than destruction of tumor vessels. |
219580-11-7 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
219580-11-7 - Introduction
PD173074 is an effective inhibitor of FGFR1, IC50 is about 25 nM, can also inhibit VEGFR2,IC50 is 100-200 nM, acting on FGFR1 is about 1000 times higher than acting on PDGFR and c-Src selectivity.
Last Update：2022-10-16 17:15:00
219580-11-7 - Reference Information
| biological activity | PD173074 is an effective FGFR1 inhibitor. in cell-free test, IC50 is about 25 nM, VEGFR2 can be inhibited, IC50 is 100-200 nM, and the selectivity of acting on FGFR1 is about 1000 times higher than that of acting on PDGFR and c-Src. PD173074 can inhibit proliferation and promote apoptosis in gastric cancer cells. |
| target | TargetValue FGFR1 (Cell-free assay) ~ 25 nM VEGFR2 (Cell-free assay) 100 nM-200 nM |
| Target | Value |
| FGFR1 (Cell-free assay) | ~25 nM |
| VEGFR2 (Cell-free assay) | 100 nM-200 nM |
| in vitro study | PD173074 is an ATP competitive inhibitor of FGFR1, K I is about 40 nM. PD173074 is also a potent inhibitor of VEGFR2. Compared with FGFR1,PD173074 weakly inhibited the activities of Src,INSR,EGFR,PDGFR,MEK and PKC, and the IC 50 value was more than 1000 times higher. PD173074 dose-dependently inhibited the autophosphorylation of FGFR1 and VEGFR2 with IC50 of 1-5 nM and 100-200 nM, respectively. PD173074 inhibit the survival of FGF-2-promoted granular neurons in a dose-dependent manner, IC50 is 12 nM, and the activity is more than 1,000 times that of SU 5402. D173074 specifically inhibit FGF-2-mediated cell proliferation, differentiation and MAPK activation of oligodendrocyte (OL) lineage cells. In multiple myeloma (MM) cell lines, PD173074 is active against wild receptors and FGFR3 mutations. PD173074 also effectively inhibited autophosphorylation of FGFR3 in a dose-dependent manner, with an IC50 of about 5 nM. PD173074 strongly reduced the viability of KMS11 cells and KMS18 cells expressing FGFR3 with IC50 less than 20 nM. PD173074 inhibition of MM cell growth stimulated by aFGF is highly related to the expression of FGFR3. PD173074 complete inhibition of NIH 3T3 transformation mediated by Y373C FGFR3 rather than Ras suggests that PD173074 specifically target cell transformation mediated by the FGFR3 gene and lack of nonspecific cytotoxic effects. PD173074 also induced functional maturation of KMS11 and KMS18 cells. |
| in vivo study | PD173074 administration to mice at 1 mg/kg/day or 2 mg/ka/day can effectively prevent angiogenesis induced by FGF or VEGF in a dose-dependent manner without obvious toxicity. PD173074 inhibit the growth of NIH 3T3 cells transfected with FGFR3 mutant in nude mice. In KMS11 xenograft tumor model, PD173074 inhibition of FGFR3 leads to delayed tumor growth and improved survival rate of mice. PD173074 blocking tumor growth and cisplatin were similar in H-510 xenografts, increasing median survival compared with control sham-treated animals. In H-69 xenografts, the induction effect of PD173074 in 50% mice was longer than 6 months. These effects are related to increased apoptosis in tumor resection, rather than destroying tumor blood vessels. |
Last Update：2024-04-09 21:04:16
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