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TL13-112
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TL13-112图片
CAS NO:2229037-19-6
包装与价格:
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

产品介绍
TL13-112 是一种有效的选择性ALK-PROTAC降解物,可抑制ALK活性,IC50值 0.14 nM,并促进包括Aurora AFERPTK2RPS6KA1在内的其他激酶的降解,IC50值分别 8550 nM、42.4 nM、25.4 nM 和 677 nM。TL13-112 由 Ceritinib (HY-15656) 和Cereblon配体 Pomalidomide (HY-10984) 结合而成。
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]

Cereblon

2.4 μM (IC50)

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]

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.
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
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM0.9974 mL4.9872 mL9.9744 mL
5 mM0.1995 mL0.9974 mL1.9949 mL
10 mM0.0997 mL0.4987 mL0.9974 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。