TL13-12

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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。

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 A、FER、PTK2和RPS6KA1，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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 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
10 mM	0.1040 mL	0.5200 mL	1.0401 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。