| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Molecular Weight (MW) | 411.89 |
|---|---|
| Formula | C20H22ClN7O |
| CAS No. | N/A |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO:>80 mg/mL |
| Water: >80 mg/mL | |
| Ethanol: >80 mg/mL | |
| Solubility (In vivo) | N/A |
| Synonyms | BAY1895344 HCl; BAY-1895344; BAY 1895344. |
| SMILES Code | CN1N=CC=C1C2=C(C=CN=C3C4=CC=NN4)C3=NC(N5[C@H](C)COCC5)=C2.[H]Cl |
| In Vitro | In vitro activity: In vitro, BAY 1895344 is a very potent and highly selective ATR inhibitor with IC50 of 7 nM. It potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC50 = 78 nM). In cellular mechanistic assays BAY 1895344 potently inhibits hydroxyurea-induced H2AX phosphorylation (IC50 = 36 nM). Kinase Assay: Elimusertib (BAY1895344) inhibits ATR with an IC50 of 7 nM. Cell Assay: In cellular mechanistic assays, BAY 1895344 inhibits hydroxyurea-induced H2AX phosphorylation. In cellular mechanistic assays BAY 1895344 potently inhibits hydroxyurea-induced H2AX phosphorylation (IC50=36 nM). |
|---|---|
| In Vivo | BAY1895344 demonstrated dramatically improved water solubility, bioavailability across species and no activity in the hERG patch-clamp assay. It also diaplays very promising efficacy in monotherapy in DNA damage deficient tumor models and in combination treatment with DNA damage inducing therapies. BAY 1895344 exhibits strong in vivo anti-tumor efficacy in monotherapy in various xenograft models of different indications that are characterized by DDR deficiencies, inducing stable disease in ovarian and colorectal cancer or even complete tumor remission in mantle cell lymphoma models. |
| Animal model | various xenograft models |
| Formulation & Dosage | NA |
| References | Cancer Research. July 2017 Volume 77, Issue 13 Supplement. |
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