2. PROTAC Apoptosis
  3. PROTACs MDM-2/p53 Apoptosis
  4. Seldegamadlin

Seldegamadlin  (Synonyms: KT-253)

目录号: HY-170451 纯度: 98.53%
COA 产品使用指南 技术支持

Seldegamadlin (KT-253) 是一种选择性 p53 稳定剂和 MDM2 PROTAC 降解剂 (DC50 = 0.4 nM)。Seldegamadlin 可抑制癌细胞 RS4;11 的增殖 (IC50 为 0.3 nM)，使细胞周期阻滞于 G2/M 期，并诱导细胞凋亡 (apoptosis)。Seldegamadlin 可上调 p53 活性并克服 p53-MDM2 反馈环路。Seldegamadlin 可用于研究血液肿瘤和实体瘤，例如急性髓系白血病 (AML) 和急性淋巴细胞白血病 (ALL)。(粉色：靶蛋白配体 MDM2 ligand 4 (HY-170452)；黑色：连接子 (HY-W001478)；蓝色：E3 连接酶 cereblon 配体 (HY-163927))。

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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Seldegamadlin

Seldegamadlin Chemical Structure

CAS No. : 2713618-08-5

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 价格 是否有货 数量
1 mg ￥3780
In-stock
5 mg 现货 询价
10 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Seldegamadlin 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC50 = 0.4 nM). Seldegamadlin inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927))[1][2][3][4].

IC50 & Target[1][2][3]

Cereblon

 

体外研究
(In Vitro)

Seldegamadlin (KT-253) 可抑制 RS4;11 ALL 细胞的活力，IC50 为 0.3 nM。KT-253 的强效生长抑制作用是通过募集 CRBN 和 MDM2 实现的[3]。
Seldegamadlin (1.8 nM；2-4 小时) 可抑制 RS4;11 ALL 细胞中 MDM2 蛋白的表达[3]。
Seldegamadlin (20 nM；2-8 小时) 可选择性地、暂时性地上调 RS4;11 ALL 细胞中 p53 及其下游靶点的表达[3]。
短暂暴露于 Seldegamadlin (1-1000 nM；4 小时) 足以诱导 RS4;11 细胞凋亡[3]。
Seldegamadlin (0.01-10000 nM；8 小时) 可有效诱导 p53 转录靶基因的表达，包括 MDM2、GDF15、CDKN1A、GADD45A、TNFRSF10B、FAS 和 BBC3[3]。
Seldegamadlin (1-1000 nM；4 小时) 可显著降低 RS4;11 和 MV4;11 细胞中处于 S 期细胞的比例[3]。
Seldegamadlin (1-10,000 nM；48-96 小时) 对多种实体瘤细胞系具有活性，包括神经母细胞瘤、横纹肌样瘤、眼瘤、胆管瘤、结直肠瘤、脂肪肉瘤、胃肉瘤、骨瘤、乳腺癌、肺癌、前列腺癌、肝瘤、脑瘤、肾瘤、甲状腺癌、膀胱癌、皮肤癌、卵巢癌、宫颈癌、子宫内膜/子宫癌、头颈部肿瘤、非癌性肿瘤和胰腺癌[4]。

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

Seldegamadlin 相关抗体:

Western Blot Analysis[3]

Cell Line: RS4;11 cells
Concentration: 1.8 nM
Incubation Time: 2 h and 4 h
Result: Led to potent and sustained MDM2 degradation to undetectable levels.

RT-PCR[3]

Cell Line: RS4;11 cells
Concentration: 20 nM
Incubation Time: 2 h, 4 h and 6 h
Result: Showed the upregulation of p53, p21 and PHLDA3.

Apoptosis Analysis[3]

Cell Line: RS4;11 cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 4 h
Result: The 4-hour treatment was sufficient to induce apoptosis over a 48-hour time frame.

Cell Cycle Analysis[3]

Cell Line: RS4;11 and MV4;11 cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 4 h
Result: Resulted in a significantly lower percentage of cells in S-phase.
体内研究
(In Vivo)

Seldegamadlin (KT-253) (1 mg/kg-10 mg/kg；静脉注射；单次) 在 RS4;11 (ALL) 和 MV-4-11 (AML) 异种移植小鼠模型中可实现持续的肿瘤消退[1]。
Seldegamadlin (1-3 mg/kg；静脉注射；单次) 可诱导 RS4;11 荷瘤小鼠的快速细胞凋亡并维持肿瘤消退[3]。
在 MOLM-13 皮下异种移植模型中，Seldegamadlin (3 mg/kg；静脉注射；单次给药) 与 Venetoclax (HY-15531) 联合用药克服了 Venetoclax 耐药性[3]。
Seldegamadlin (3-10 mg/kg；静脉注射；每 3 周一次) 在多种 PDX 实体瘤模型中抑制肿瘤生长，并达到完全缓解[4]。

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

Animal Model: Immuno-compromised host strain mice were subcutaneous with RS4;11 (ALL) cell lines[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: IV; once
Result: Achieved sustained tumor regression in RS4;11 xenograft model.
Led to rapid increase in p53, p21 and PUMA (1 mg/kg).
Animal Model: Female Balb/c nude mice were subcutaneously MV4;11 cells in the hind flank of the animals.[3]
Dosage: 1 mg/kg, 3 mg/kg
Administration: IV; once
Result: Induced tumor regressions.
Demonstrated robust degradation of MDM2.
Showed an upregulation of proteomic biomarkers p53, p21, and PHLDA3.
Revealed robust upregulation of p53 and induction of apoptosis, as indicated by cleaved caspase-3 (CC-3) staining.
Led to robust activation of mRNA markers of both the intrinsic (BBC3) and extrinsic (TNFRSF10B and FAS) apoptotic pathways.
Animal Model: Twenty-fourpediatric patient-derived xenograft (PDX) models (Ewing sarcoma, rhabdomyosarcoma, rhabdoid tumor,Wilms tumor, hepatoblastoma, and neuroblastoma, breast, lung,colorectal, gastric, melanoma) [4]
Dosage: 3 mg/kg, 10 mg/kg
Administration: IV; Q3W; total 3 dose
Result: Inhibited tumor growth in pediatric solid tumor models, achieving complete responses in 9 out of 24 models.
Animal Model: Immuno-compromised host strain mice were subcutaneous with MV-4-11 (AML) cell lines[1]
Dosage: 3 mg/kg
Administration: IV; once every 3 weeks
Result: Achieved sustained tumor regression in MV-4-11 xenograft model.
Led to rapid increase in GDF15, p21 and PUMA.
Clinical Trial
分子量

912.87

Formula

C48H52Cl2FN7O6
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, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 95 mg/mL (104.07 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 1.0954 mL 5.4772 mL 10.9545 mL
5 mM 0.2191 mL 1.0954 mL 2.1909 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 (protect from 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

Seldegamadlin 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 (protect from 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 1.0954 mL 5.4772 mL 10.9545 mL 27.3862 mL
5 mM 0.2191 mL 1.0954 mL 2.1909 mL 5.4772 mL
10 mM 0.1095 mL 0.5477 mL 1.0954 mL 2.7386 mL
15 mM 0.0730 mL 0.3651 mL 0.7303 mL 1.8257 mL
20 mM 0.0548 mL 0.2739 mL 0.5477 mL 1.3693 mL
25 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0954 mL
30 mM 0.0365 mL 0.1826 mL 0.3651 mL 0.9129 mL
40 mM 0.0274 mL 0.1369 mL 0.2739 mL 0.6847 mL
50 mM 0.0219 mL 0.1095 mL 0.2191 mL 0.5477 mL
60 mM 0.0183 mL 0.0913 mL 0.1826 mL 0.4564 mL
80 mM 0.0137 mL 0.0685 mL 0.1369 mL 0.3423 mL
100 mM 0.0110 mL 0.0548 mL 0.1095 mL 0.2739 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:

Seldegamadlin2713618-08-5KT-253KT253KT 253PROTACsMDM-2/p53ApoptosisUveal melanomabiological activitypotencyxenograft modelAMLsmall molecule inhibitorssolid tumorstumor cell killingp53 stabilizationwildtype p53 tumorsprotein degradationapoptosisMDM2hematologic tumorsautoregulatory feedback loopSMItumor regressionMDM2 degraderp53venetoclax resistancetumor suppressionInhibitorinhibitorinhibit

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：
Seldegamadlin
目录号：
HY-170451
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