CS-1804
OSI-930
CAS: 728033-96-3
Molecular Formula: C22H16F3N3O2S
CS-1804 - Names and Identifiers
CS-1804 - Physico-chemical Properties
| Molecular Formula | C22H16F3N3O2S |
| Molar Mass | 443.44 |
| Density | 1.450 |
| Boling Point | 517.4±50.0 °C(Predicted) |
| pKa | 11.36±0.70(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | In vitro, OSI-930 effective inhibition of recombinant receptor tyrosine kinase activity, acting on Kit, KDR, Flt, CSF-1R, c-Raf and Lck, IC50 80 nM, 9 nM, 8 nM, 15 nM, 41 nM and 22 nM. OSI-930 acts on the HMC-1 cell line to inhibit cell proliferation with an IC50 of 14 nM, but acts on COLO-205 cells that do not express the constitutively activated mutant receptor tyrosine kinase, and does not significantly inhibit growth. Furthermore, OSI-930 also induced apoptosis in HMC-1 cells with an EC50 of 34 nM. A recent study showed that OSI-930 inactivated the purified recombinant cytochrome P450 (P450) 3A4 with K I of 24 μm in a time-and concentration-dependent manner. |
| In vivo study | OSI-930 according to the maximum effective dose of 200 mg/kg oral feeding treatment administration of a variety of preclinical model of transplanted tumor. Including HMC-1, NCI-SNU-5, COLO-205 and U251 transplanted tumor model, has effective anti-tumor activity. |
CS-1804 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.255 ml | 11.275 ml | 22.55 ml |
| 5 mM | 0.451 ml | 2.255 ml | 4.51 ml |
| 10 mM | 0.226 ml | 1.128 ml | 2.255 ml |
| 5 mM | 0.045 ml | 0.226 ml | 0.451 ml |
Last Update：2024-01-02 23:10:35
CS-1804 - Reference Information
| biological activity | OSI-930 is an effective Kit (c-Kit), KDR and CSF-1R inhibitor with IC50 of 80 nM, 9 nM and 15 nM respectively. it has moderate inhibitory activity on Flt-1, c-Raf and Lck, and weak inhibitory activity on PDGFRα/β, Flt-3 and Abl. Phase 1. |
| target | TargetValue FLT1 (Cell-Free Assay) 8 nM KDR (Cell-Free Assay) 9 nM CSF-1R (Cell-Free Assay) 15 nM LCK (Cell-Free Assay) 22 nM C- Raf (Cell-Free Assay) 41 nM |
| Target | Value |
| FLT1 (Cell-free assay) | 8 nM |
| KDR (Cell-free assay) | 9 nM |
| CSF-1R (Cell-free assay) | 15 nM |
| LCK (Cell-free assay) | 22 nM |
| C-Raf (Cell-free assay) | 41 nM |
| in vitro study | in vitro, OSI-930 effectively inhibit the activity of recombinant receptor tyrosine kinase. when acting on Kit, KDR, Flt, CSF-1R, c-Raf and Lck, the IC50 is 80 nM, 9 nM, 8 nM, 15 nM, 41 nM and 22 nM respectively. OSI-930 acts on HMC-1 cell lines to inhibit cell proliferation with IC50 of 14 nM, while acting on COLO-205 cells that do not express constitutively activated mutant receptor tyrosine kinase will not significantly inhibit growth. Moreover, OSI-930 also induced apoptosis of HMC-1 cells with EC50 of 34 nM. The latest research shows that OSI-930 inactivates purified recombinant cytochrome P450 (P450) 3A4 with K I of 24 μM, which is time-and concentration-dependent. |
| in vivo study | OSI-930 was treated with oral feeding at the maximum effective dose of 200 mg/kg for various preclinical transplanted tumor models. Including HMC-1, NCI-SNU-5, COLO-205 and U251 transplanted tumor models, it has effective anti-tumor activity. |
Last Update：2024-04-09 21:54:55
Supplier List
Product Name: OSI-930 Visit Supplier Webpage Request for quotation
CAS: 728033-96-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 728033-96-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: OSI-930 Visit Supplier Webpage Request for quotation
CAS: 728033-96-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 728033-96-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History