1009820-21-6
CX-4945 (Silmitasertib)
CAS: 1009820-21-6
Molecular Formula: C19H12ClN3O2
1009820-21-6 - Names and Identifiers
1009820-21-6 - Physico-chemical Properties
| Molecular Formula | C19H12ClN3O2 |
| Molar Mass | 349.77 |
| Density | 1.490 |
| Boling Point | 568.5±50.0 °C(Predicted) |
| Appearance | Orange powder. |
| pKa | 2.96±0.30(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | CX-4945 is a specific inhibitor of CK2, which inhibits only 7 of the 238 kinases and its inhibition rate is more than 0.5 at a concentration of 90% μm, which is more than 500 times the IC50 of ck2. While CX-4945 inhibition of FLT3, PIM1, and CDK1 in cell-free systems has an IC50 of 35 nM, 46 nM, and 56 nM, respectively, however, the inhibition of FLT3, PIM1 and CDK1 by CX-4945 at 10 μm was not strong in cell-based functional experiments. CX-4945 has a broad spectrum of anti malignant cell proliferation activity. Breast cancer cell lines were most extensively sensitive to CX-4945, with EC50 of 1.71-20.01 μm. CX-4945 anti-malignant cell proliferation activity corresponded to CK2α mRNA and protein levels, but was not associated with CK2α' catalytic subunit, modulation of CK2β subfamily, and PI3K/Akt or PTEN mutation status. CX-4945 inhibition of the PI3K/Akt signaling pathway by inhibiting CK2 directly blocks phosphorylation of Akt at serine 129, rather than by inhibiting activated PTEN. Treatment with CX-4945 resulted in a decrease in phosphorylated p21 (T145), while overall levels of p21 and p27 were elevated, inducing caspase 3/7 activity. Treatment with CX-4945 induced BT-474 cell block in the G2/M phase of the cell cycle and BxPC-3 cell block in the G1 phase. CX-4945 inhibited the proliferation, migration and angiogenesis of HUVEC with IC50 of 5.5 μm, 2 μm and 4 μm, respectively. Treatment of BT-474 in BxPC-3 and CX-4945 cells under hypoxic conditions blocked p53 and pVHL down-regulation and reduced the transcriptional activity of HIF-1α. The activity of endogenous CK2 in Jurkat cells was effectively inhibited by CX-4945 in endogenous cells with an IC50 of 0.1 μm. |
| In vivo study | In the BT-474 model, oral administration of CX-4945 at 25 mg/kg or 75 mg/kg twice a day had potent anticancer activity with TGI of 88% and 97%, respectively, in 2 out of 9 experimental animals in each group, the size of the tumor volume was reduced by 50% compared with the initial one. In the BxPC-3 model, treated twice a day with 75 mg/kg of CX-4945, TGI was 93%, and at the end of the treatment period, no residual tumors were noted in 3 animals. In PC3 xenograft models, treatment with CX-4945 at 25 mg/kg, 50 mg/kg, or 75 mg/kg inhibited tumor growth with TGI of 19%, 40%, and 86%, respectively |
1009820-21-6 - Risk and Safety
| HS Code | 29339900 |
1009820-21-6 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.859 ml | 14.295 ml | 28.59 ml |
| 5 mM | 0.572 ml | 2.859 ml | 5.718 ml |
| 10 mM | 0.286 ml | 1.43 ml | 2.859 ml |
| 5 mM | 0.057 ml | 0.286 ml | 0.572 ml |
Last Update：2024-01-02 23:10:35
1009820-21-6 - Reference Information
| biological activity | Silmitasertib (CX-4945) is effective, selective CK2(casein kinase 2) inhibitor, IC50 is 1 nM in cell-free test, and the effect on Flt3, Pim1 and CDK1 is slightly weak (no activity in cell test). Silmitasertib can induce autophagy and promote cell apoptosis. Phase 1/2. |
| target | TargetValue CK2 (Cell-free say) 1 nM |
| Target | Value |
| CK2 (Cell-free assay) | 1 nM |
| in vitro study | CX-4945 is a specific inhibitor of CK2. it only inhibits 7 of 238 kinases and its inhibition rate exceeds 90% at 0.5 μM concentration, which is more than 500 times of IC50 of CK2. While the IC50 for CX-4945 inhibition of FLT3, PIM1, and CDK1 was 35 nM, 46 nM, and 56 nM, respectively, in cell-free systems, a 10 μM CX-4945 was not strong in inhibition of FLT3, PIM1, and CDK1 in cell-based functional experiments. CX-4945 has broad-spectrum anti-malignant cell proliferation activity. Breast cancer cell lines are most sensitive to CX-4945, with EC50 of 1.71-20.01 μM. The anti-malignant cell proliferation activity of CX-4945 corresponds to CK2α mRNA and protein levels, but is not related to CK2α' catalytic subunit, adjustment of CK2β subfamily and PI3K/Akt or PTEN mutation status. CX-4945 inhibits the PI3K/Akt signaling pathway by inhibiting CK2 directly blocking the phosphorylation of serine at position 129 of Akt, rather than by inhibiting activated PTEN. Treatment with CX-4945 can cause a decrease in phosphorylation of p21 (T145), while the overall levels of p21 and p27 will increase, while inducing caspase 3/7 activity. Treatment with CX-4945 induces BT-474 cells to block in G2/M phase of the cell cycle and BxPC-3 cells to block in G1 phase. CX-4945 can inhibit the proliferation, migration and angiogenesis of HUVEC, and its IC50 is 5.5 μM, 2 μM and 4 μM respectively. Treatment of BT-474 and BxPC-3 cells with CX-4945 at low oxygen content can block the down-regulation of p53 and pVHL and reduce the transcriptional activity of HIF-1α. CX-4945 in Jurkat cells can effectively inhibit the activity of endogenous CK2 in endogenous cells, and its IC50 is 0.1 μM. |
| in vivo study | in BT-474 model, CX-4945 with 25 mg/kg or 75 mg/kg orally twice a day has strong anti-cancer activity, TGI is 88% and 97% respectively, the size of tumors in 2 out of 9 experimental animals in each group was reduced by 50% compared with the initial one. In the BxPC-3 model, treated with 75 mg/kg CX-4945 twice a day, TGI was 93%. At the end of the treatment period, 3 animals did not find any residual tumor. In the PC3 xenograft model, treatment with 25 mg/kg, 50 mg/kg or 75 mg/kg CX-4945 can inhibit tumor growth, TGI is 19%, 40% and 86% |
Last Update：2024-04-09 21:11:58
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Product Name: 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid Visit Supplier Webpage Request for quotationCAS: 1009820-21-6
Tel: +86-400-900-4166
Email: product@acmec-e.com
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Tel: 609-228-6898
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