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CDK6/PIM1-IN-1

CAS: 2677026-14-9 F: C25H28FN9 W: 473.55

CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/
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Bioactivity 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].
Invitro CDK6/PIM1-IN-1 (compound 51) exhibits more than 10 times selectivity over CDK1 (IC50>10 μM), CDK2 (IC50=2.274 μM), CDK3 (IC50>10 μM), CDK5 (IC50>10 μM), CDK7 (IC50=393 nM), CDK9 (IC50=440 nM), CDK12 (IC50>10 μM), and CDK13 (IC50>10 μM). CDK6/PIM1-IN-1 shows inhibitory activity against PIM2 (IC50>10 μM) and PIM3 (IC50=92 nM)[1]. CDK6/PIM1-IN-1 inhibits proliferation in AML cells (K562 cell,GI50=1.026 μM; HL-60 cell,GI50=1.069 μM; MOLM13 cell, GI50=1.362 μM)[1]. CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM) causes a G1 arrest in a dose-dependent manner in K562 and HL-60 cell lines[1]. CDK6/PIM1-IN-1 (1, 2, 4 μM) promotes the apoptosis of K562 and HL-60 cell lines in a dose-dependent manner[1]. CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM; for 24 h) reduces p-retinoblastoma (RB) and p-BAD levels in a concentration-dependent manner. CDK6/PIM1-IN-1 decreases the PIM1 level[1].
Name CDK6/PIM1-IN-1
CAS 2677026-14-9
Formula C25H28FN9
Molar Mass 473.55
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.