2. PROTAC Apoptosis
  3. PROTACs Bcl-2 Family Apoptosis
  4. PZ671

PZ671 是一种强效的针对 Bcl-xL 的 PROTAC 靶向降解剂，在 MOLT-4 细胞中的 IC50 为 1.3 nM，对 Bcl-xL 的 DC50 为 0.9 nM。PZ671 能够诱导 MOLT-4 细胞凋亡 (apoptosis)。PZ671 能有效抑制 MOLT-4 异种移植小鼠中肿瘤的生长并能够迅速恢复血小板数目短暂性的降低。PZ671 可用于癌症研究，如小细胞肺癌。(结构：粉色：Bcl-xL ligand (HY-174878)；蓝色; CRBN Ligand (HY-138793)；黑色：连接子；E3-连接子偶联物 (HY-174879))

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PZ671 Chemical Structure

PZ671 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

PZ671 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PZ671 is a potent Bcl-xL PROTAC degrader with an IC50 of 1.3 nM (MOLT-4 cells) and a DC50 of 0.9 nM (Bcl-xL). PZ671 induces apoptosis in MOLT-4 cells. PZ671 effectively inhibits tumor growth and rapidly reverses transient platelet counts reduction in MOLT-4 xenograft mice. PZ671 can be used for the research of cancer, such as small cell lung cancer (SCLC)[1]. (Structure Note: Pink: Bcl-xL ligand (HY-174878); Blue: CRBN Ligand (HY-138793); Black: linker; E3-linker (HY-174879))

IC50 & Target[1]

Bcl-xL

 

Cereblon

 

体外研究
(In Vitro)

PZ671 (Compound 5b) (0.4-100 nM, 1-16 h) 可诱导 MOLT-4 细胞中 Bcl-xL 降解[1]。

PZ671 (10, 100 nM) 在 MOLT-4 细胞中通过蛋白酶体依赖途径降解 Bcl-xL[1]。

PZ671 (0.4-100 nM, 48 h) 可诱导 MOLT-4 细胞凋亡[1]。

PZ671 (30-1000 nM, 48 h) 在浓度高于 1 μM 时会引起人血小板中 Bcl-xL 降解[1]。

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

PZ671 相关抗体:

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 0.4, 1, 3, 11, 33. and 100 nM
Incubation Time: 16 h, and 100 nM for 1, 2, 3, 4, 5, 6 h
Result: Induced dose-dependent Bcl-xL degradation in MOLT-4 cells.
Significantly reduced Bcl-xL levels within 2 h, and almost complete degradation of Bcl-xL after 4 h at 100 nM.

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 10 and 100 nM, pretreatingt with 1 μM MG-132 (HY-13259) for 2 h
Incubation Time: /
Result: Degradation was blocked by proteasome inhibitor MG-132 (HY-13259).

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 0.4, 1, 3, 11, 33. and 100 nM
Incubation Time: 16 h
Result: Dose-dependently increased poly (ADP-ribose) polymerase (PARP) and caspase-3 cleavage.
Significantly reduced β-actin levels with increasing concentrations.

Western Blot Analysis[1]

Cell Line: Human platelets
Concentration: 30, 100, 300 and 1000 nM
Incubation Time: 48 h
Result: Degraded Bcl-xL at concentrations above 1 μM.
体内研究
(In Vivo)

PZ671 (1.5 mg/kg；腹腔注射；每 4 天一次，持续 22 天) 在 MOLT-4 异种移植小鼠中显著抑制了肿瘤生长，但给药后引起血小板计数短暂下降，从第二天起能迅速恢复[1]。

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

Animal Model: MOLT-4 xenograft mice (CB-17 SCID, Female, 5-6 weeks)[1]
Dosage: 1.5 mg/kg
Administration: Intraperitoneal injection, every 4 days for 22 days
Result: Markedly suppressed the tumor growth.
Caused a transient ∼72% reduction in platelet counts after a single dose, with rapid recovery from the second day onward.
分子量

1335.02

Formula

C66H79ClF3N7O11S3
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PZ671 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

PZ671PZ 671PZ-671PROTACsBcl-2 FamilyApoptosisBcl-xLSmall cell lung cancerMOLT-4 cellsMOLT-4 xenograft miceInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
PZ671
目录号：
HY-174876
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z