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| IC86621 Basic information |
| IC86621 Chemical Properties |
| Melting point | 98-100.3 °C | | Boiling point | 425.5±45.0 °C(Predicted) | | density | 1.210±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: 15 mg/mL | | pka | 10.47±0.10(Predicted) | | form | solid | | color | off-white |
| IC86621 Usage And Synthesis |
| General Description | A cell-permeable aryl-morpholino compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 120 nM) and PI 3-Kinase catalytic subunit p110β (IC50 = 135 nM). It inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC50 = 68 μM) and enhances DSB-induced antitumor activity both in vitro and in vivo, while exhibiting no cytotoxic effects (up to 50 μM) in the absence of DSBs. It inhibits PI 3-K p110α, p110γ, and p110δ only at much higher concentrations (IC50 = 1.4, 0.88, and 1.0 μM, respectively) and exhibits no effect against a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 μM. | | Biochem/physiol Actions | Cell permeable: yes |
| IC86621 Preparation Products And Raw materials |
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