2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Btk
  4. PROTAC BTK Degrader-1

PROTAC BTK Degrader-1 

目录号: HY-147943 纯度: 98.87%
COA 产品使用指南

摩尔计算器

PROTAC BTK Degrader-1 是一种有效且具有选择性和口服活性的 PROTAC BTK 降解剂，对野生型 BTK 和突变型 BTK-481S 的IC50 分别为 34.51 nM 和 64.56 nM。PROTAC BTK Degrader-1 能有效降低 BTK 蛋白水平，抑制肿瘤生长。

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PROTAC BTK Degrader-1 Chemical Structure

PROTAC BTK Degrader-1 Chemical Structure

CAS No. : 2801715-13-7

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规格 价格 是否有货 数量
1 mg ￥1916
In-stock
5 mg ￥3833
In-stock
10 mg ￥5750
In-stock
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100 mg   询价  

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Customer Review

PROTAC BTK Degrader-1 相关抗体

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth[1]. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

IC50: 34.51 nM (BTK WT), 64.56 nM (BTK-481S)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
JeKo-1 IC50
104.69 nM
Compound: C13
Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
[PMID: 35671249]
JeKo-1 IC50
708.2 nM
Compound: C13
Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
[PMID: 35671249]
OCI-Ly10 IC50
5.9 nM
Compound: C13
Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
[PMID: 35671249]
TMD8 IC50
4.7 nM
Compound: C13
Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
[PMID: 35671249]
体内研究
(In Vivo)

PROTAC BTK Degrader-1 (compound C13) (10 and 30 mg/kg; PO, bid, for 17 days) inhibits tumor growth in the OCI-ly10 xenograft mouse model[1].
Pharmacokinetic Parameters of PROTAC BTK Degrader-1 in ICR mice[1].

PO (100 mg/kg) IV (2 mg/kg)
Tmax (h) 1.00
T1/2 (h) 8.3 3.7
Cmax (ng/mL) 3089
AUC0-t (ng/mL·h) 16,894 2827
AUC0-∞ (ng/mL·h) 17,070 2845
VdSS (L/kg) 3.1
CL (mL/min/kg) 11.7
MRT (h) 4.5
F (%) 12

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

Animal Model: OCI-ly10 xenograft mouse model[1]
Dosage: 10 and 30 mg/kg
Administration: PO, bid, for 17 days
Result: Inhibited tumor growth by 50.9 and 96.9% at 10 and 30 mg/kg, respectively.
分子量

749.86

Formula

C43H43N9O4
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (133.36 mM; 超声助溶; 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 1.3336 mL 6.6679 mL 13.3358 mL
5 mM 0.2667 mL 1.3336 mL 2.6672 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 (sealed storage, away from moisture and light)。-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

只
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

PROTAC BTK Degrader-1 相关分类

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 (sealed storage, away from moisture and light)。-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 1.3336 mL 6.6679 mL 13.3358 mL 33.3396 mL
5 mM 0.2667 mL 1.3336 mL 2.6672 mL 6.6679 mL
10 mM 0.1334 mL 0.6668 mL 1.3336 mL 3.3340 mL
15 mM 0.0889 mL 0.4445 mL 0.8891 mL 2.2226 mL
20 mM 0.0667 mL 0.3334 mL 0.6668 mL 1.6670 mL
25 mM 0.0533 mL 0.2667 mL 0.5334 mL 1.3336 mL
30 mM 0.0445 mL 0.2223 mL 0.4445 mL 1.1113 mL
40 mM 0.0333 mL 0.1667 mL 0.3334 mL 0.8335 mL
50 mM 0.0267 mL 0.1334 mL 0.2667 mL 0.6668 mL
60 mM 0.0222 mL 0.1111 mL 0.2223 mL 0.5557 mL
80 mM 0.0167 mL 0.0833 mL 0.1667 mL 0.4167 mL
100 mM 0.0133 mL 0.0667 mL 0.1334 mL 0.3334 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.

Keywords:

PROTAC BTK Degrader-12801715-13-7PROTAC BTK Degrader1PROTAC BTK Degrader 1PROTACsBtkBruton tyrosine kinaseanticancerantitumororally activeOCI-ly10xenograftICR miceInhibitorinhibitorinhibit

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