2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Anaplastic lymphoma kinase (ALK)
  4. TL13-12

TL13-12 is a potent and selective?ALK-PROTAC?degrader and inhibits?ALK?activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984).

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TL13-12 Chemical Structure

TL13-12 Chemical Structure

CAS No. : 2229037-04-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 600 In-stock
25 mg USD 1250 In-stock
50 mg USD 1950 In-stock
100 mg USD 3200 In-stock
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Based on 1 publication(s) in Google Scholar

TL13-12 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

TL13-12 is a potent and selective?ALK-PROTAC?degrader and inhibits?ALK?activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984)[1].

IC50 & Target

Cereblon

1.2 μM (IC50)

In Vitro

TL13-12 (0-200 nM; 16 hours) ?is selective for degradation of ALK with the DC50s of 10 nM and 180 nM in H3122 cell and Karpas 299, respectively[1].
TL13-12 (0-160 nM; 16 hours) degrades ALK and aurora A protein expression as a dose-dependent manner in Kelly and CHLA20 cells[1].
TL13-12 (100 nM; 16 hours) significantly inhibits Tariqudan-induced ALK and Aurora A protein expression in CHLA20 cells[1].

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

TL13-12 Related Antibodies

Western Blot Analysis[1]

Cell Line: Kelly and CHLA20 cells
Concentration: 0 nM; 20 nM; 40 nM; 60 nM; 80 nM; 100 nM; 140 nM; 160 nM
Incubation Time: 16 hours
Result: Exhibited degrader behavior in cells.

Western Blot Analysis[1]

Cell Line: CHLA20 cells
Concentration: 100 nM
Incubation Time: 16 hours
Result: Decreased ALK and Aurora A protein expression.
Molecular Weight

961.48

Formula

C45H53ClN10O10S
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

O=C(NCCOCCOCCN1CCN(C2=CC=C(NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3)C(OC)=C2)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 (104.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0401 mL 5.2003 mL 10.4006 mL
5 mM 0.2080 mL 1.0401 mL 2.0801 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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In Vivo Dissolution Calculator
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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 1.0401 mL 5.2003 mL 10.4006 mL 26.0016 mL
5 mM 0.2080 mL 1.0401 mL 2.0801 mL 5.2003 mL
10 mM 0.1040 mL 0.5200 mL 1.0401 mL 2.6002 mL
15 mM 0.0693 mL 0.3467 mL 0.6934 mL 1.7334 mL
20 mM 0.0520 mL 0.2600 mL 0.5200 mL 1.3001 mL
25 mM 0.0416 mL 0.2080 mL 0.4160 mL 1.0401 mL
30 mM 0.0347 mL 0.1733 mL 0.3467 mL 0.8667 mL
40 mM 0.0260 mL 0.1300 mL 0.2600 mL 0.6500 mL
50 mM 0.0208 mL 0.1040 mL 0.2080 mL 0.5200 mL
60 mM 0.0173 mL 0.0867 mL 0.1733 mL 0.4334 mL
80 mM 0.0130 mL 0.0650 mL 0.1300 mL 0.3250 mL
100 mM 0.0104 mL 0.0520 mL 0.1040 mL 0.2600 mL
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TL13-12 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:

TL13-122229037-04-9PROTACsAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ALKPROTACKellyCHLA20 H3122Karpas 299Inhibitorinhibitorinhibit

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