CAS NO: | 2229037-19-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | 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]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | 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]. Western Blot Analysis[1]
Western Blot Analysis[1]
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分子量 | 1002.57 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C49H60ClN9O10S | ||||||||||||||||
CAS 号 | 2229037-19-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(99.74 mM;ultrasonic and warming and heat to 60℃) 配制储备液
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