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TL12-186
CAS No. 2250025-88-6
TL12-186( —— )
Catalog No. M34721 CAS 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.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 258 | In Stock |
|
| 2MG | 91 | In Stock |
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| 5MG | 150 | In Stock |
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| 10MG | 236 | In Stock |
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| 25MG | 377 | In Stock |
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| 50MG | 529 | In Stock |
|
| 100MG | 731 | In Stock |
|
| 200MG | 1004 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameTL12-186
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NoteResearch use only, not for human use.
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Brief DescriptionTL12-186 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.
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DescriptionTL12-186 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).
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In VitroCell Proliferation Assay 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 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.
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In Vivo——
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Synonyms——
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PathwayOthers
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TargetOther Targets
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RecptorPROTACs | CDK
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Research Area——
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Indication——
Chemical Information
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CAS Number2250025-88-6
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Formula Weight931.46
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Molecular FormulaC44H51ClN10O9S
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 200 mg/mL (214.72 mM; Ultrasonic )
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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
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Hai-Tsang Huang, et al.A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader. Cell Chem Biol. 2018 Jan 18;25(1):88-99.e6.?
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