ICEC 0942 hydrochloride

Research use only, not for human use.

ICEC 0942 (CT7001) is a potent, selective, orally active CDK7 inhibitor with IC50 of 41 nM, displays 15-fold selectivity over CDK2 (IC50=578 nM).

ICEC 0942 (CT7001) is a potent, selective, orally active CDK7 inhibitor with IC50 of 41 nM, displays 15-fold selectivity over CDK2 (IC50=578 nM); displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2, CDK5 and CDK9; demonstrates sensitivity against a wide range of cancer types with GI50 values ranging between 0.2-0.3 uM; shows substantial anti-tumor effects in xenografts of both breast and colorectal cancers, also exhibits complete growth arrest of ER-positive tumor xenografts combined with tamoxifen.Solid Tumors Phase 1 Clinical.

Apoptosis Analysis Cell Line:HCT116 cells Concentration:0 μM, 0.1 μM, 1 μM and 10 μM Incubation Time:24 hours Result:Induced caspase 3/7 and demonstrated PARP cleavage.Cell Cycle Analysis Cell Line:HCT116 cells Concentration:0 μM, 0.01 μM, 0.1 μM, 1 μM and 10 μM Incubation Time:24 hours Result:Showed accumulation of cells in G2/M.Western Blot Analysis Cell Line:HCT116 cells Concentration:0 μM, 0.1 μM, 1 μM and 10 μM Incubation Time:0 hour, 4 hours, 8 hours, 16 hours or 24 hours Result:PolII CTD phosphorylation was inhibited in a dose and time dependent manner in HCT116 colon cancer cells.

Animal Model:Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells Dosage:100 mg/kg Administration:Oral gavage; daily; for 14 days Result:At day 14, tumor growth was inhibited by 60%.

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Cell Cycle/DNA Damage

CDK

CDK

Cancer

Solid Tumors

1805789-54-1

430.981

C22H31ClN6O

>98% (HPLC)

DMSO : ≥ 62.5 mg/mL 145.02 mM

CC(C)C1=C2N=C(C=C(N2N=C1)NCC3=CC=CC=C3)NCC4CCNCC4O.Cl

(3R,4R)-4-(((7-(benzylamino)-3-isopropylpyrazolo[1,5-a]pyrimidin-5-yl)amino)methyl)piperidin-3-ol hydrochloride

(-20℃)

With Ice Pack

≥ 2 years