1089283-49-7
gsk 1904529a
CAS: 1089283-49-7
Molecular Formula: C44H47F2N9O5S
1089283-49-7 - Names and Identifiers
1089283-49-7 - Physico-chemical Properties
| Molecular Formula | C44H47F2N9O5S |
| Molar Mass | 851.96 |
| Density | 1.39 |
| pKa | 11.12±0.70(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | GSK1904529A is a selective inhibitor with IC50 of 27 and 25 nM for IGF-IR and IR, respectively. GSK1904529A is a reversible ATP competitive inhibitor. The K I values for GSK1904529A at IGF-IR and IR were 1.3 and 1.6 nM, respectively. GSK1904529A effectively inhibited IGF-IR and IR phosphorylation at concentrations greater than 0.01 μm and subsequently blocked downstream signaling. Cell Proliferation experiments showed that GSK1904529A effectively inhibited NIH-3T3/LISN, TC-71, SK-N-MC, SK-ES, and RD-ES cells with IC50 of 60, 35, 43, 61, and 62 nM, respectively. GSK1904529A also inhibits other multiple myeloma and Ewing's sarcoma cell lines, including NCI-H929, MOLP-8, LP-1, and KMS-12-BM, among others. |
| In vivo study | Mice carrying NIH-3T3/LISN tumor were treated orally with 30mg GSK1904529A per kilogram of body weight twice a day, and the tumor inhibition rate was 98%, treatment once a day showed a tumor inhibition rate of 75%. GSK1904529A can be used to treat a variety of IGF-IR-dependent tumors, including prostate, colon, breast, pancreatic, ovarian, and sarcoma. |
1089283-49-7 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.174 ml | 5.869 ml | 11.738 ml |
| 5 mM | 0.235 ml | 1.174 ml | 2.348 ml |
| 10 mM | 0.117 ml | 0.587 ml | 1.174 ml |
| 5 mM | 0.023 ml | 0.117 ml | 0.235 ml |
Last Update：2024-01-02 23:10:35
1089283-49-7 - Reference Information
| biological activity | GSK1904529A (GSK 4529) is a selective IGF-1R and IR inhibitor. in the cell-free test, IC50 is 27 nM and 25 nM respectively, acting on IGF-1R/InsR ratio acting on Akt1/2/, Aurora A/B,B-Raf, CDK2, EGFR and other selectivity is more than 100 times higher. |
| target | TargetValue Insulin Receptor (Cell-free assay) 25 nM IGF-1R (Cell-free assay) 27 nM |
| Target | Value |
| Insulin Receptor (Cell-free assay) | 25 nM |
| IGF-1R (Cell-free assay) | 27 nM |
| in vitro study | GSK1904529A are selective inhibitors, and IC50 is 27 and 25 nM respectively when acting on IGF-IR and IR. GSK1904529A is a reversible ATP competitive inhibitor. When the GSK1904529A acts on IGF-IR and IR, the K I values are 1.3 and 1.6 nM respectively. GSK1904529A concentrations greater than 0.01 μM effectively inhibit IGF-IR and IR phosphorylation, and then block downstream signals. Cell proliferation experiments showed that GSK1904529A effectively inhibited NIH-3T3/LISN, TC-71, SK-N-MC, SK-ES, and RD-ES cells with IC50 of 60, 35, 43, 61, and 62 nM respectively. GSK1904529A also inhibits other multiple myeloma and Ewing's sarcoma cell lines, including NCI-H929, MOLP-8, LP-1, and KMS-12-BM. |
| in vivo study | mice carrying NIH-3T3/LISN tumors were orally treated with 30mg of GSK1904529A per kilogram according to their body weight twice a day, and the results showed that the tumor inhibition rate was 98%. However, GSK1904529A acts on mice carrying COLO 205 transplanted tumors and is treated once a day, the results showed that the tumor inhibition rate was 75%. GSK1904529A can be used to treat a variety of IGF-IR-dependent tumors, including prostate cancer, colon cancer, breast cancer, pancreatic cancer, ovarian cancer, and sarcoma. |
Last Update：2024-04-09 21:49:45
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Product Name: GSK1904529A Visit Supplier Webpage Request for quotation
CAS: 1089283-49-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1089283-49-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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