1. Cell Cycle/DNA Damage
  2. CDK
  3. SEL120-34A

SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Romaciclib monohydrochloride and Romaciclib hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

SEL120-34A Chemical Structure

SEL120-34A Chemical Structure

CAS No. : 1609522-33-9

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Description

SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

IC50 & Target[1]

CDK8/CycC

4.4 nM (IC50)

CDK19/CycC

10.4 nM (IC50)

CDK9/cycT

1070 nM (IC50)

In Vitro

SEL120-34A is a selective, ATP-competitive CDK8 inhibitor, with IC50 of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively. SEL120-34A shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC50, 1070 nM). SEL120-34A is active against a panel of AML cell lines (GI50<1 μM), such as SKNO-1, KG-1, HEL-60, MOLM-16, MV-4-11, OciAML-2, MOLM-6 and OciAML-3 cells, consistent with the effective inhibition range of STAT1 S727 and STAT5 S726[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SEL120-34A (30, 60 mg/kg, p.o.) inhibits the growth of tumor in mice bearing MV4-11 cancer cells, and also arrests the growth of KG-1-derived tumors at 30 mg/kg via oral administration[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

414.14

Formula

C15H18Br2N4

CAS No.
SMILES

CC1=C2C3=C(C(Br)=C1Br)CCCN3C(N4CCNCC4)=N2

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SEL120-34A
Cat. No.:
HY-111388
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