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TL12-186

🥰Excellent
Catalog No. T34888Cas No. 2250025-88-6
Alias TL12186, TL12 186

TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively.

TL12-186

TL12-186

🥰Excellent
Purity: 98.2%
Catalog No. T34888Alias TL12186, TL12 186Cas No. 2250025-88-6
TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively.
Pack SizePriceAvailabilityQuantity
1 mg$116In Stock
5 mg$288In Stock
10 mg$482In Stock
25 mg$892In Stock
50 mg$1,220In Stock
100 mg$1,650In Stock
1 mL x 10 mM (in DMSO)$490In Stock
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Purity:98.2%
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Product Introduction

Bioactivity
Description
TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively.
Targets&IC50
CDK2-CyclinA:73 nM (IC50), CRBN:12nM, CDK9-CyclinT1:55 nM (IC50)
In vitro
TL12-186 demonstrates over 90% inhibition against 193 kinases at a screening concentration of 1 μM[1]. Utilizing AlphaScreen binding assays, it exhibits potent binding to CRBN with an IC50 of 12 nM[1]. Displaying CRBN-dependent pharmacological effects, TL12-186 (1-10000 nM; 2 days) exerts 13 to 15 times stronger inhibition of cell survival in WT cells compared to CRBN-/- cells[1]. Moreover, at concentrations ranging from 10 to 10000 nM for 4 hours, TL12-186 selectively inhibits STAT1 phosphorylation without inducing degradation of JAK1/2[1].
AliasTL12186, TL12 186
Chemical Properties
Molecular Weight931.46
FormulaC44H51ClN10O9S
Cas No.2250025-88-6
SmilesO=C1NC(=O)C(N2C(=O)C=3C=CC=C(NCC(=O)NCCOCCOCCN4CCN(C5=CC=C(C=C5)NC6=NC=C(Cl)C(=N6)NC=7C=CC=CC7S(=O)(=O)C(C)C)CC4)C3C2=O)CC1
Relative Density.no data available
Storage & Solubility Information
Storagekeep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 200 mg/mL (214.72 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.0736 mL5.3679 mL10.7358 mL53.6792 mL
5 mM0.2147 mL1.0736 mL2.1472 mL10.7358 mL
10 mM0.1074 mL0.5368 mL1.0736 mL5.3679 mL
20 mM0.0537 mL0.2684 mL0.5368 mL2.6840 mL
50 mM0.0215 mL0.1074 mL0.2147 mL1.0736 mL
100 mM0.0107 mL0.0537 mL0.1074 mL0.5368 mL

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