Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CDK/HDAC-IN-3 is an orally active dual inhibitor of HDACs and CDKs, offering potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3, with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM, respectively. This compound is applicable in the treatment of acute myeloid leukemia (AML) [1].
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
25 mg | 約8-10 週間 | ¥ 452,500 |
50 mg | 約8-10 週間 | ¥ 592,500 |
100 mg | 約8-10 週間 | ¥ 780,500 |
説明 | CDK/HDAC-IN-3 is an orally active dual inhibitor of HDACs and CDKs, offering potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3, with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM, respectively. This compound is applicable in the treatment of acute myeloid leukemia (AML) [1]. |
In vitro | CDK/HDAC-IN-3 (compound 33a) at 1μM demonstrates potent and selective inhibition against CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM respectively [1]. At concentrations of 0.5 μM and 1.0 μM, this compound significantly induces differentiation of leukemia stem cell-like cells and inhibits the proliferation of AML [1]. Additionally, CDK/HDAC-IN-3 at 0.5 μM, 1.0 μM, and 2.0 μM markedly promotes differentiation of LSCs [1]. The compound also exhibits inhibitory effects on U937, HL-60, SKNO-1, and Kasumi-1 cells with IC50 values of 0.72 μM, 1.43 μM, 1.63 μM, and 0.89 μM respectively [1]. |
In vivo | CDK/HDAC-IN-3 (compound 33a), when administered intravenously (i.v.) or orally (p.o.) at doses of 5 mg/kg and 25 mg/kg, exhibits good oral bioavailability [1]. |
分子量 | 509.34 |
分子式 | C24H18Cl2N6O3 |
CAS No. | 2944087-54-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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CDK/HDAC-IN-3 2944087-54-9 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Inhibitor inhibitor inhibit