1. Cell Cycle/DNA Damage
  2. CDK

SEL120-34A HCl 

Cat. No.: HY-111388B Purity: 99.80%
Handling Instructions

SEL120-34A HCl 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.

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

SEL120-34A HCl Chemical Structure

SEL120-34A HCl Chemical Structure

CAS No. : 1609452-30-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 330 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Other Forms of SEL120-34A HCl:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

SEL120-34A HCl 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 HCl 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 HCl shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC50, 1070 nM). SEL120-34A HCl 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].

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].

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (Need ultrasonic)

In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (Infinity mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2.08 mg/mL (Infinity mM); Clear solution; Need warming

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (Infinity mM); Clear solution

References
Formula

C₁₅H₁₈Br₂N₄.xHCl

CAS No.

1609452-30-3

SMILES

CC1=C(Br)C(Br)=C2C3=C1N=C(N4CCNCC4)N3CCC2.[x HCl]

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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

Cat. No.: HY-111388B