2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Anaplastic lymphoma kinase (ALK)
  4. TL13-112

TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib (HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984).

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

TL13-112 Chemical Structure

TL13-112 Chemical Structure

CAS No. : 2229037-19-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 651 In-stock
Solution
10 mM * 1 mL in DMSO USD 651 In-stock
Solid
5 mg USD 380 In-stock
10 mg USD 590 In-stock
25 mg USD 1180 In-stock
50 mg USD 1900 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

TL13-112 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE TL13-112

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib (HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984)[1].

IC50 & Target[1]

Cereblon

2.4 μM (IC50)

In Vitro

TL13-112 binds to cereblon with an IC50 value of 2.4 uM[1].
TL13-112 (0.01 μM-1 μM; 16 hours) is selective for degradation of ALK with the DC50s of 10 nM and 40 nM in H3122 cell and Karpas 299, respectively. ALK degradation acts at 4 hours of treatment in H3122 cells and at 8 hours of treatment in Karpas 299 cells. The maximum degradation achieves at 16 hours in both cell lines. [1].
TL13-112 (0.01 μM-1 μM; 16 hours) inhibits PTK2, ALK, FER, RPS6KA1 and Aurora A expression as a dose-dependent manner in H3122, Karpas 299, and Kelly cells[1].

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

TL13-112 Related Antibodies

Western Blot Analysis[1]

Cell Line: H3122 and Karpas 299 cells
Concentration: 0.01 μM; 0.05 μM; 0.1 μM; 0.5 μM; 1 μM
Incubation Time: 16 hours
Result: Inhibited ALK and Aurora A expression completely at 1 μM.

Western Blot Analysis[1]

Cell Line: H3122 and Karpas 299 cells
Concentration: 0.01 μM; 0.05 μM; 0.1 μM; 0.5 μM; 1 μM
Incubation Time: 16 hours
Result: Decreased PTK2, ALK, FER, RPS6KA1 and Aurora A expression.
Molecular Weight

1002.57

Formula

C49H60ClN9O10S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCCOCCOCCN1CCC(C2=CC(OC(C)C)=C(NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3)C=C2C)CC1)CNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (99.74 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9974 mL 4.9872 mL 9.9744 mL
5 mM 0.1995 mL 0.9974 mL 1.9949 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9974 mL 4.9872 mL 9.9744 mL 24.9359 mL
5 mM 0.1995 mL 0.9974 mL 1.9949 mL 4.9872 mL
10 mM 0.0997 mL 0.4987 mL 0.9974 mL 2.4936 mL
15 mM 0.0665 mL 0.3325 mL 0.6650 mL 1.6624 mL
20 mM 0.0499 mL 0.2494 mL 0.4987 mL 1.2468 mL
25 mM 0.0399 mL 0.1995 mL 0.3990 mL 0.9974 mL
30 mM 0.0332 mL 0.1662 mL 0.3325 mL 0.8312 mL
40 mM 0.0249 mL 0.1247 mL 0.2494 mL 0.6234 mL
50 mM 0.0199 mL 0.0997 mL 0.1995 mL 0.4987 mL
60 mM 0.0166 mL 0.0831 mL 0.1662 mL 0.4156 mL
80 mM 0.0125 mL 0.0623 mL 0.1247 mL 0.3117 mL
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TL13-112 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TL13-1122229037-19-6PROTACsAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246cereblonH3122Karpas 299KellycanceralkInhibitorinhibitorinhibit

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