CDK12-IN-E9
CAS No. : 2020052-55-3
| Size | Price | Stock |
|---|---|---|
| 5mg | $400 | In-stock |
| 10mg | $600 | In-stock |
| 25mg | $1125 | In-stock |
| 50mg | $1800 | In-stock |
| 100mg | $2700 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-117203A |
| M.Wt: | 434.53 |
| Formula: | C24H30N6O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 125 mg/mL (ultrasonic) |
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM[1].
In Vitro: CDK12-IN-E9 (E9; 10 nM-10 μM; 72 hours; Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells) treatment shows potent antiproliferative activity in THZ1R NB and lung cancer cells, with IC50 values ranging from 8 to 40 nM[1].
CDK12-IN-E9 (E9; 0-3000 nM; 6 hours; Kelly, PC-9, and NCI-H82 cells) treatment leads to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1r NB and lung cancer models, accompanied by decreased MYC and MCL1 expression[1].
CDK12-IN-E9 also results in increased PARP cleavage, and an increase in the subGI population in THZ1r lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9[1].
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