(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-pyrrolidinecarboxamide BMS 754807
BMS-754807
CAS: 1001350-96-4
Molecular Formula: C23H24FN9O
(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-pyrrolidinecarboxamide BMS 754807 - Names and Identifiers
(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-pyrrolidinecarboxamide BMS 754807 - Physico-chemical Properties
| Molecular Formula | C23H24FN9O |
| Molar Mass | 461.49 |
| Density | 1.58 |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | room temp |
| In vitro study | BMS-754807 effectively inhibits the growth of tumor cell lines of various human tissue origins, including mesenchymal (Ewing's sarcoma, rhabdomyosarcoma, neuroblastoma, and liposarcoma), epithelial (breast, lung, pancreas, colon, and stomach), and hematopoietic (multiple myeloma and leukemia) tissues, with IC50 values ranging from 5 nM to 365 nM. BMS-754807 inhibited the proliferation of IGF-1R-Sal cells and RH41 cells with IC50 of 7 nM and 5 nM, respectively. BMS-754807 inhibited IGF-1R-Sal phosphorylation in IGF-1R, Rh41 and Geo cells with IC50 of 13 nM, 6 nM and 21 nM, respectively. BMS-754807 inhibits Akt phosphorylation in IGF-1R-Sal, Rh41 and Geo cells with IC50 of 22 nM, 13 nM and 16 nM, respectively. BMS-754807 induced apoptosis of Rh41 cells. BMS-754807 inhibited IGF-Sal (IC50 = 13nM) and downstream targets Akt (IC50 = 22nM) and MAPK(IC50 = 13nM) in IGF-1R cell line. Phosphorylation. In the pediatric preclinical program (PPTP), 23 cell lines were treated BMS-754807 with a mean EC50 value of 0.62 μm. BMS-754807 effectively inhibits the growth of tumor cell lines of various human tissue origins, including mesenchymal (Ewing's sarcoma, rhabdomyosarcoma, neuroblastoma, and liposarcoma), epithelial (breast, lung, pancreas, colon, and stomach), and hematopoietic (multiple myeloma and leukemia) tissues with IC50 values ranging from 5 nM to 365 nM. BMS-754807 inhibited the proliferation of IGF-1R-Sal cells and RH41 cells with IC50 of 7 nM and 5 nM, respectively. BMS-754807 inhibited IGF-1R-Sal phosphorylation in IGF-1R, Rh41 and Geo cells with IC50 of 13 nM, 6 nM and 21 nM, respectively. BMS-754807 inhibits Akt phosphorylation in IGF-1R-Sal, Rh41 and Geo cells with IC50 of 22 nM, 13 nM and 16 nM, respectively. BMS-754807 induced apoptosis of Rh41 cells. BMS-754807 acts on the IGF-Sal cell line and inhibits phosphorylation of IGF-1R (IC50 = 13nm) and downstream targets Akt (IC50 = 22nm) and MAPK(IC50 = 13nm). In the pediatric preclinical program (PPTP), 23 cell lines were treated BMS-754807 with a mean EC50 value of 0.62 μm. |
| In vivo study | BMS-754807(12.5mg/kg, oral) in nude mice carrying IGF-1R-Sal tumor, tumor and serum IGF-1R phosphorylation. BMS-754807 inhibits tumor growth in a selected set of epithelial (IGF-1R-Sal, GEO, and Colo205), hematopoietic (JJN3) and mesenchymal (RD1 and Rh41) xenograft models, tumor growth inhibition rates ranged from 53% to 115%. BMS-754807 (6.25 mg/kg) completely inhibited tumor growth and inhibited IGF-Sal and pAKT in the transgenic pIGF-1R tumor mouse model. The protein binding rates to mouse plasma and human plasma BMS-754807 were 98.5% and 95.9%, respectively. BMS-754807 (25 mg/kg) significantly inhibited tumors in a mouse model carrying KT-5 (Wilms), KT-14 (rhabdoid), Rh28 (rhabdomyosarcoma), and OS-1 xenografts. BMS-754807(12.5mg/kg, P. O.) inhibited IGF-1R-Sal phosphorylation of tumor and serum in nude mice with IGF-1R tumor. BMS-754807 inhibits tumor growth in a selected set of epithelial (IGF-1R-Sal, GEO, and Colo205), hematopoietic (JJN3) and mesenchymal (RD1 and Rh41) xenograft models, tumor growth inhibition rates ranged from 53% to 115%. BMS-754807 (6.25 mg/kg) completely inhibited tumor growth and inhibited IGF-Sal and pAKT in the transgenic pIGF-1R tumor mouse model. The protein binding rates to mouse plasma and human plasma BMS-754807 were 98.5% and 95.9%, respectively. BMS-754807 (25 mg/kg) significantly inhibited tumors in a mouse model carrying KT-5 (Wilms), KT-14 (rhabdoid), Rh28 (rhabdomyosarcoma), and OS-1 xenografts. |
(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-pyrrolidinecarboxamide BMS 754807 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.167 ml | 10.834 ml | 21.669 ml |
| 5 mM | 0.433 ml | 2.167 ml | 4.334 ml |
| 10 mM | 0.217 ml | 1.083 ml | 2.167 ml |
| 5 mM | 0.043 ml | 0.217 ml | 0.433 ml |
Last Update：2024-01-02 23:10:35
(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-pyrrolidinecarboxamide BMS 754807 - Reference Information
| biological activity | BMS-754807 is a potent IGF-1R/InsR reversible inhibitor with IC50 of 1.8 nM/1.7 nM, the effect on Met, Aurora A/B, TrkA/B and Ron was slightly weak, and there was almost no inhibitory activity on Flt3, Lck, MK2, PKA, PKC, etc. Phase 2. BMS-754807 is A potent IGF-1R/InsR reversible inhibitor with an IC50 of 1.8 nM/1.7 nM in A cell-free assay versus Met (c-Met),Aurora A/B, trkA/B and Ron had little inhibitory activity on Flt3, Lck,MK2,PKA,PKC, etc. Phase 2. |
| in vitro study | BMS-754807 effectively inhibits the growth of a variety of human tumor cell lines derived from different tissues, including mesenchymal (Ewing's sarcoma, rhabdomyosarcoma, neuroblastoma, and liposarcoma), epithelial (breast, lung, pancreas, colon, and stomach), and hematopoietic (multiple myeloma and leukemia) tissues with IC50 values from 5 nM to 365 nM. BMS-754807 inhibited the proliferation of IGF-1R-Sal cells and RH41 cells with IC50 of 7 nM and 5 nM, respectively. BMS-754807 inhibited IGF-1R-Sal phosphorylation in IGF-1R, Rh41 and Geo cells with IC50 of 13 nM, 6 nM and 21 nM, respectively. BMS-754807 inhibits Akt phosphorylation in IGF-1R-Sal, Rh41 and Geo cells with IC50 of 22 nM, 13 nM and 16 nM, respectively. BMS-754807 induced apoptosis of Rh41 cells. BMS-754807 inhibited IGF-Sal (IC50 = 13nM) and downstream targets Akt (IC50 = 22nM) and MAPK(IC50 = 13nM) in IGF-1R cell line. Phosphorylation. In the pediatric preclinical program (PPTP), 23 cell lines were treated BMS-754807 with a mean EC50 value of 0.62 μm. BMS-754807 effectively inhibits the growth of tumor cell lines of various human tissue origins, including mesenchymal (Ewing's sarcoma, rhabdomyosarcoma, neuroblastoma, and liposarcoma), epithelial (breast, lung, pancreas, colon, and stomach), and hematopoietic (multiple myeloma and leukemia) tissues with IC50 values ranging from 5 nM to 365 nM. BMS-754807 inhibited the proliferation of IGF-1R-Sal cells and RH41 cells with IC50 of 7 nM and 5 nM, respectively. BMS-754807 inhibited IGF-1R-Sal phosphorylation in IGF-1R, Rh41 and Geo cells with IC50 of 13 nM, 6 nM and 21 nM, respectively. BMS-754807 inhibits Akt phosphorylation in IGF-1R-Sal, Rh41 and Geo cells with IC50 of 22 nM, 13 nM and 16 nM, respectively. BMS-754807 induced apoptosis of Rh41 cells. BMS-754807 acts on the IGF-Sal cell line and inhibits phosphorylation of IGF-1R (IC50 = 13nm) and downstream targets Akt (IC50 = 22nm) and MAPK(IC50 = 13nm). In the pediatric preclinical program (PPTP), 23 cell lines were treated BMS-754807 with a mean EC50 value of 0.62 μm. |
| in vivo study | BMS-754807(12.5mg/kg, oral) in nude mice with IGF-1R-Sal tumor, inhibition of IGF-1R phosphorylation in tumor and serum. BMS-754807 inhibits tumor growth in a selected set of epithelial (IGF-1R-Sal, GEO, and Colo205), hematopoietic (JJN3) and mesenchymal (RD1 and Rh41) xenograft models, tumor growth inhibition rates ranged from 53% to 115%. BMS-754807 (6.25 mg/kg) completely inhibited tumor growth and inhibited IGF-Sal and pAKT in the transgenic pIGF-1R tumor mouse model. The protein binding rates to mouse plasma and human plasma BMS-754807 were 98.5% and 95.9%, respectively. BMS-754807 (25 mg/kg) significantly inhibited tumors in a mouse model carrying KT-5 (Wilms), KT-14 (rhabdoid), Rh28 (rhabdomyosarcoma), and OS-1 xenografts. BMS-754807(12.5mg/kg, P. O.) inhibited IGF-1R-Sal phosphorylation of tumor and serum in nude mice with IGF-1R tumor. BMS-754807 inhibits tumor growth in a selected set of epithelial (IGF-1R-Sal, GEO, and Colo205), hematopoietic (JJN3) and mesenchymal (RD1 and Rh41) xenograft models, tumor growth inhibition rates ranged from 53% to 115%. BMS-754807 (6.25 mg/kg) completely inhibited tumor growth and inhibited IGF-Sal and pAKT in the transgenic pIGF-1R tumor mouse model. The protein binding rates to mouse plasma and human plasma BMS-754807 were 98.5% and 95.9%, respectively. BMS-754807 (25 mg/kg) significantly inhibited tumors in a mouse model carrying KT-5 (Wilms), KT-14 (rhabdoid), Rh28 (rhabdomyosarcoma), and OS-1 xenografts. |
| characteristics | multiple inhibitors of insulin-like growth factor-1r/IR family kinases |
| Target | TargetValue Insulin Receptor (Cell-free assay) 1.7 nM IGF-1R (Cell-free assay) 1.8 nM TrkB (Cell-free assay) 4.1 nM Met (Cell-free assay) 5.6 nM TrkA (Cell-free assay) 7.4 nM |
| Target | Value |
| Insulin Receptor (Cell-free assay) | 1.7 nM |
| IGF-1R (Cell-free assay) | 1.8 nM |
| TrkB (Cell-free assay) | 4.1 nM |
| Met (Cell-free assay) | 5.6 nM |
| TrkA (Cell-free assay) | 7.4 nM |
Last Update：2024-04-09 20:45:29
![(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-pyrrolidinecarboxamide BMS 754807](http://res.chembk.com/assets/images/structure/300011.gif)
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Spot supply
Product Name: BMS 754807 Visit Supplier Webpage Request for quotationCAS: 1001350-96-4
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: BMS-754807 Visit Supplier Webpage Request for quotationCAS: 1001350-96-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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