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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 Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $116 | In Stock | |
5 mg | $288 | In Stock | |
10 mg | $482 | In Stock | |
25 mg | $892 | In Stock | |
50 mg | $1,220 | In Stock | |
100 mg | $1,650 | In Stock | |
1 mL x 10 mM (in DMSO) | $490 | In Stock |
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]. |
Alias | TL12186, TL12 186 |
Molecular Weight | 931.46 |
Formula | C44H51ClN10O9S |
Cas No. | 2250025-88-6 |
Smiles | O=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 | keep 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
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