1. PROTAC
    Cell Cycle/DNA Damage
  2. PROTACs
    CDK
  3. TL12-186

TL12-186 

Cat. No.: HY-130665 Purity: 98.05%
Handling Instructions

TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM).

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

TL12-186 Chemical Structure

TL12-186 Chemical Structure

CAS No. : 2250025-88-6

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 605 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 590 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM)[1].

IC50 & Target[1]

Cereblon

 

cdk2/cyclin A

73 nM (IC50)

CDK9/cyclinT1

55 nM (IC50)

In Vitro

TL12-186 displays >90% inhibition of 193 kinases at a screening concentration of 1 μM[1].
TL12-186 displays potent binding to CRBN (IC50=12 nM) using an AlphaScreen engagement assay[1].
TL12-186 (1-10000 nM; 2 days) exhibits a CRBN-dependent pharmacological effect, displaying 13 to 15-fold more potent inhibition of survival of the WT cells than the CRBN-/- cells[1].
TL12-186 (10-10000 nM; 4 hours) inhibits STAT1 phosphorylation without causing JAK1/2 degradation[1].

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

Cell Proliferation Assay[1]

Cell Line: WT and CRBN-/- MOLM-14 cells; WT and CRBN-/- MOLT-4 cells
Concentration: 1, 10, 100, 1000, 10000 nM
Incubation Time: 2 days
Result: Exhibited a CRBN-dependent pharmacological effect, displaying 13 to 15-fold more potent inhibition of survival of the WT cells than the CRBN-/- cells.

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 4 hours
Result: Inhibited IFN-γ (10 ng/mL)-stimulated STAT1 phosphorylation (Y701) without causing degradation of JAK1 or JAK2.
Molecular Weight

931.46

Formula

C44H51ClN10O9S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (214.72 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0736 mL 5.3679 mL 10.7358 mL
5 mM 0.2147 mL 1.0736 mL 2.1472 mL
10 mM 0.1074 mL 0.5368 mL 1.0736 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 5 mg/mL (5.37 mM); Clear solution

  • 2.

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

    Solubility: ≥ 5 mg/mL (5.37 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: ≥99.0%

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Product Name:
TL12-186
Cat. No.:
HY-130665
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