1. PROTAC Protein Tyrosine Kinase/RTK
  2. PROTACs Anaplastic lymphoma kinase (ALK)
  3. TL13-112

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。

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TL13-112 Chemical Structure

TL13-112 Chemical Structure

CAS No. : 2229037-19-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥6510
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1 mg ¥1727
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5 mg ¥3800
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10 mg ¥5900
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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values 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 the Cereblon ligand 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 IC50 value 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C49H60ClN9O10S

CAS 号
性状

固体

颜色

Light yellow to yellow

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
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (99.74 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9974 mL 4.9872 mL 9.9744 mL
5 mM 0.1995 mL 0.9974 mL 1.9949 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9974 mL 4.9872 mL 9.9744 mL 24.9359 mL
5 mM 0.1995 mL 0.9974 mL 1.9949 mL 4.9872 mL
10 mM 0.0997 mL 0.4987 mL 0.9974 mL 2.4936 mL
15 mM 0.0665 mL 0.3325 mL 0.6650 mL 1.6624 mL
20 mM 0.0499 mL 0.2494 mL 0.4987 mL 1.2468 mL
25 mM 0.0399 mL 0.1995 mL 0.3990 mL 0.9974 mL
30 mM 0.0332 mL 0.1662 mL 0.3325 mL 0.8312 mL
40 mM 0.0249 mL 0.1247 mL 0.2494 mL 0.6234 mL
50 mM 0.0199 mL 0.0997 mL 0.1995 mL 0.4987 mL
60 mM 0.0166 mL 0.0831 mL 0.1662 mL 0.4156 mL
80 mM 0.0125 mL 0.0623 mL 0.1247 mL 0.3117 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
TL13-112
目录号:
HY-123919
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