2677026-14-9

Name	2-Quinoxalinamine, N,N-diethyl-7-[5-fluoro-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-4-pyrimidinyl]-
CAS	2677026-14-9
Molecular Formula	C25H28FN9
Molecular Weight	473.55
MOL File	2677026-14-9.mol

Synonyms

CDK6/PIM1-IN-1 2-Quinoxalinamine, N,N-diethyl-7-[5-fluoro-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-4-pyrimidinyl]-

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Chemical Properties

Boiling point	716.9±70.0 °C(Predicted)
density	1.299±0.06 g/cm3(Predicted)
pka	8.63±0.10(Predicted)

Hazard Information

Uses

CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50?values of 39 and 88 nM, respectively.?CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity[1].

in vivo

CDK6/PIM1-IN-1 (compound 51; orally; 60, 90 mg/kg/day; 17 days) displays more potent antitumor activity?in BALB/c mice with K562 cell lines^[1].
CDK6/PIM1-IN-1 (iv; 5 mg/kg) has the t_1/2, MRT_0-∞, and AUC_0-∞?values of 9.78 h, 14.61 h, and 1153.74 h·ng/mL, respectively in Sprague–Dawley (SD) rats^[1].
CDK6/PIM1-IN-1 (po; 5 mg/kg) has the?t_1/2, T_max, C_max, and AUC_0-∞ of 15.81 h, 11 h, 152.31 ng/mL, and 5152.92 h·ng/mL, respectively in SD rats^[1].

IC 50

CDK6/cyclinD1: 39 nM (IC₅₀); CDK1/cyclinB: >10 μM (IC₅₀); CDK2/cyclinA: 2.274 μM (IC₅₀); CDK3/Cyclin E: >10 μM (IC₅₀); Cdk4/cyclin D1: 3.6 nM (IC₅₀); Cdk5/p25: >10 μM (IC₅₀); CDK7/Cyclin H/MNAT1: 393 nM (IC₅₀); CDK9/cyclinT1: 440 nM (IC₅₀); CDK12/Cyclin K: >10 μM (IC₅₀); CDK13/Cyclin K: >10 μM (IC₅₀); PIM1: 88 nM (IC₅₀); PIM2: >10 μM (IC₅₀); PIM3: 92 nM (IC₅₀)

References

[1] Kai Yuan, et al. Discovery of Dual CDK6/PIM1 Inhibitors with a Novel Structure, High Potency, and Favorable Druggability for the Treatment of Acute Myeloid Leukemia. J Med Chem. 2022 Jan 13;65(1):857-875. DOI:10.1021/acs.jmedchem.1c02019

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