2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs CDK
  4. PROTAC CDK2-pRb degrader-1

PROTAC CDK2-pRb degrader-1 是一种口服有效的 PRTOAC 类 CDK2/cyclin E 的降解剂。PROTAC CDK2-pRb degrader-1 能够通过诱导 CDK2 的泛素化及蛋白酶体降解，有效抑制视网膜母细胞瘤蛋白 (Rb) 在丝氨酸残基 807/811 位点的磷酸化。PROTAC CDK2-pRb degrader-1 对人源细胞表现出显著的活性 (EC50 值分别为 12 nM 和 125 nM)。在异种移植模型中，PROTAC CDK2-pRb degrader-1 能有效抑制肿瘤生长并诱导肿瘤停滞，适用于 CCNE1 扩增型癌症 (如卵巢癌、胃癌、乳腺癌) 的相关研究。

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PROTAC CDK2-pRb degrader-1

PROTAC CDK2-pRb degrader-1 Chemical Structure

CAS No. : 3030276-48-0

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PROTAC CDK2-pRb degrader-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer)[1].

IC50 & Target

CDK2/cyclinE

 

体外研究
(In Vitro)

PROTAC CDK2-pRb degrader-1 (Compound 5) (剂量反应浓度；24 h) 可同时降解 CDK2 和 Cyclin E1，在 CCNE1 扩增的人类癌细胞系中活性增强，并且能在过表达 Cyclin E1 的 Palbociclib (HY-50767) 适应性乳腺癌细胞中恢复 RB 通路的抑制作用[1]。
PROTAC CDK2-pRb degrader-1 (剂量响应浓度；7 天) 在 MKN1 和 HCC1569 人癌细胞系中展现出依赖于 CRBN 的抗增殖活性[1]。
PROTAC CDK2-pRb degrader-1 (剂量响应浓度；7 天) 在依赖功能性 RB 蛋白的 HCC1569 人乳腺癌细胞中表现出抗增殖活性[1]。

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

PROTAC CDK2-pRb degrader-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MKN1 (CRBNwt, CRBNKO), HCC1569 (CRBNwt, CRBNKO)
Concentration: dose-response concentrations
Incubation Time: 7 days
Result: Lost antiproliferative activity in CRBNKO MKN1 and HCC1569 cells, with proliferation largely restored compared to CRBNwt cells where the degrader potently suppressed growth.

Cell Proliferation Assay[1]

Cell Line: HCC1569 (RBwt, RBKO)
Concentration: dose-response concentrations
Incubation Time: 7 days
Result: Showed >300-fold reduced antiproliferative potency in RBKO HCC1569 cells compared to RBwt cells.
体内研究
(In Vivo)

PROTAC CDK2-pRb degrader-1 (50 mg/kg；口服；每日两次) 可在 OVCAR3 CCNE1 扩增型卵巢癌异种移植物中实现近 90% 的 pRB 抑制率和 85% 的肿瘤生长抑制率 (接近停滞)[1]。
PROTAC CDK2-pRb degrader-1 (50 mg/kg；口服；每日 2 次) 可诱导肿瘤停滞或消退；在 CCNE1 扩增的 HCC1569 乳腺癌异种移植模型中，能实现 90% 的 CDK2 降解及 pRB 抑制[1]。
PROTAC CDK2-pRb degrader-1 (50 mg/kg；口服；每日 1 次) 可诱导肿瘤停滞或消退；在 CCNE1 扩增的 MKN1 胃癌异种移植模型中，可实现 90% 的 CDK2 降解及 pRB 抑制[1]。

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

Animal Model: NOD SCID (female)[1]
Dosage: 50 mg/kg
Administration: p.o.; BID
Result: Inhibited nearly 90% of phosphorylated Rb (pRB) in tumor tissue, with decreased rebound of pRB signal at trough compared to PF-07104091 (HY-137894A).
Induced potent tumor growth inhibition (TGI) of 85%.
Animal Model: NOG (female)[1]
Dosage: 15 mg/kg; 30 mg/kg; 50 mg/kg
Administration: p.o.; BID
Result: Achieved sustained 90% CDK2 degradation and 90% pRB inhibition in tumor tissue at 30 and 50 mg/kg BID.
Induced tumor stasis with 95% TGI at 30 mg/kg compared to vehicle.
Induced 5% tumor regression at 50 mg/kg compared to vehicle.
Animal Model: BALB/c Nude (female)[1]
Dosage: 30 mg/kg; 50 mg/kg
Administration: p.o.; QD
Result: Induced 90% CDK2 degradation and 90% pRB inhibition in tumor tissue at 50 mg/kg QD.
Induced tumor stasis (TGI=97%) at 30 mg/kg compared to vehicle.
Induced 47% tumor regression at 50 mg/kg compared to vehicle.
分子量

830.93

Formula

C40H50F4N8O5S
CAS 号
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

PROTAC CDK2-pRb degrader-1 相关分类

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  • 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 CDK2-pRb degrader-13030276-48-0PROTACsCDKCyclin dependent kinaseproteasomal degradationCDK2ubiquitinationCCNE1-amplified cancersovarian cancerbreast cancercyclin E1xenograft modelsretinoblastoma protein (Rb)gastric cancerInhibitorinhibitorinhibit

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