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TL13-12
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。
TL13-12图片
CAS NO:2229037-04-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
TL13-12 是一种强效的ALK-PROTAC降解物,抑制ALK活性,其IC50值为 0.69 nM,并促进其他激酶的降解,包括Aurora AFERPTK2RPS6KA1,其IC50值分别为 13.5 nM、5.74 nM、18.4 nM 和 65 nM。TL13-12 由 TAE684 (HY-10192) 和Cereblon配体 Pomalidomide (HY-10984) 结合而成。
生物活性

TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with anIC50value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases includingAurora A,FER,PTK2, andRPS6KA1withIC50values 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 theCereblonligand of Pomalidomide (HY-10984)[1].

IC50& Target

Cereblon

1.2 μM (IC50)

体外研究
(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].

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.
分子量

961.48

性状

Solid

Formula

C45H53ClN10O10S

CAS 号

2229037-04-9

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(104.01 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.0401 mL5.2003 mL10.4006 mL
5 mM0.2080 mL1.0401 mL2.0801 mL
10 mM0.1040 mL0.5200 mL1.0401 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。