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Biochem/physiol Actions
ETP-46464 is a potent and selective inhibitor of the DNA damage response kinase Ataxia telangiectasia-mutated (ATM) - and Rad3-related (ATR) with an IC50 of 25 nM. ETP-46464 shows moderate activity against PI3K and is a potent inhibitor of mTor, but is selective for ATR versus ATM and DNA -dependent protein kinase (DNA -PKcs) even at high doses. ETP-46464 inhibited phosphorylation of Chk1, the downstream kinase of ATR, but did not affect ionizing radiation–induced γH2AX formation, which is jointly controlled by ATM and DNA-PKc.
ETP-46464 is a potent and selective inhibitor of the DNA damage response kinase Ataxia telangiectasia-mutated (ATM) - and Rad3-related (ATR).
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to light brown |
| solubility | DMSO: 2 mg/mL, clear (warmed) |
| web metadata keyword.default | ATAXIA telangiectasia mutated inhibitor ETP-46464,ATR selective inhibitor ETP-46464,DNA damage response kinase inhibitor ETP-46464,ETP-46464 1345675-02-6,ETP-46464 25 nM IC50 inhibitor,ETP-46464 Chk1 phosphorylation inhibitor,ETP-46464 chemical structure and properties,ETP-46464 for cancer research applications,ETP-46464 for research,ETP-46464 inhibitor,ETP-46464 mTor inhibitor for lab use,ETP-46464 research-grade,ETP-46464,Sigma-Aldrich ETP-46464 |
| storage temp. | −20°C |
| SMILES string | CC(C)(C#N)C(C=C1)=CC=C1N(C2=C(CO3)C=NC(C2=C4)=CC=C4C5=CC6=C(C=CC=C6)N=C5)C3=O |
| InChI | 1S/C30H22N4O2/c1-30(2,18-31)23-8-10-24(11-9-23)34-28-22(17-36-29(34)35)16-33-27-12-7-19(14-25(27)28)21-13-20-5-3-4-6-26(20)32-15-21/h3-16H,17H2,1-2H3 |
| InChI key | DPLMXAYKJZOTKO-UHFFFAOYSA-N |
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