TL13-112 is a potent and selectiveALK-PROTACdegrader and inhibitsALKactivity with anIC₅₀value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases includingAurora A,FER,PTK2andRPS6KA1withIC₅₀values 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 theCereblonligand of Pomalidomide (HY-10984)^[1].

TL13-112 binds to cereblon with an IC₅₀value 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].

1002.57

Solid

C₄₉H₆₀ClN₉O₁₀S

2229037-19-6

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL(99.74 mM;ultrasonic and warming and heat to 60℃)

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