1. PROTAC Protein Tyrosine Kinase/RTK
  2. PROTACs Anaplastic lymphoma kinase (ALK)
  3. TL13-12

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。

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TL13-12 Chemical Structure

TL13-12 Chemical Structure

CAS No. : 2229037-04-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3850
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1 mg ¥1590
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5 mg ¥3500
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10 mg ¥6000
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values 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 the Cereblon ligand 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].

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

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

Formula

C45H53ClN10O10S

CAS 号
性状

固体

颜色

Yellow to brown

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 中的溶解度 : ≥ 100 mg/mL (104.01 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" 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
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 1.0401 mL 5.2003 mL 10.4006 mL 26.0016 mL
5 mM 0.2080 mL 1.0401 mL 2.0801 mL 5.2003 mL
10 mM 0.1040 mL 0.5200 mL 1.0401 mL 2.6002 mL
15 mM 0.0693 mL 0.3467 mL 0.6934 mL 1.7334 mL
20 mM 0.0520 mL 0.2600 mL 0.5200 mL 1.3001 mL
25 mM 0.0416 mL 0.2080 mL 0.4160 mL 1.0401 mL
30 mM 0.0347 mL 0.1733 mL 0.3467 mL 0.8667 mL
40 mM 0.0260 mL 0.1300 mL 0.2600 mL 0.6500 mL
50 mM 0.0208 mL 0.1040 mL 0.2080 mL 0.5200 mL
60 mM 0.0173 mL 0.0867 mL 0.1733 mL 0.4334 mL
80 mM 0.0130 mL 0.0650 mL 0.1300 mL 0.3250 mL
100 mM 0.0104 mL 0.0520 mL 0.1040 mL 0.2600 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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Inquiry Information

产品名称:
TL13-12
目录号:
HY-122582
需求量: