2. Cell Cycle/DNA Damage
  3. CDK
  4. Cyclin A/B RxL-IN-1

Cyclin A/B RxL-IN-1 是一种靶向 Cyclin A/B RxL 与疏水斑块 (HP) 相互作用的抑制剂。Cyclin A/B RxL-IN-1 对 Cyclin A 的抑制作用的 IC50 为 0.12 μM。Cyclin A/B RxL-IN-1 在小鼠细胞系来源的异种移植瘤 (CDX) 模型中表现出抗肿瘤疗效。CDK-IN-19 可用于研究 E2F 驱动的癌症，如小细胞肺癌 (SCLC)。

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Cyclin A/B RxL-IN-1

Cyclin A/B RxL-IN-1 Chemical Structure

CAS No. : 3036231-62-3

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Cyclin A/B RxL-IN-1 相关抗体

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cyclin A/B RxL-IN-1 is a inhibitor targeting the Cyclin A/B RxL interaction at the hydrophobic patch (HP). Cyclin A/B RxL-IN-1 inhibits Cyclin A with an IC50 of 0.12 μM. Cyclin A/B RxL-IN-1 demonstrates antitumor efficacy in mouse cell line-derived xenograft (CDX) models. CDK-IN-19 can be used for the study of E2F-driven cancers such as small-cell lung cancer (SCLC)[1].

体外研究
(In Vitro)

Cyclin A/B RxL-IN-1 (Compound 34) (5 days) 抑制 RB1/E2F 失调的小细胞肺癌 (SCLC) 细胞增殖，在 NCI-H69 细胞和 NCI-H1048 细胞中的 GI50 分别为 0.016 μM 和 0.048 μM[1]。
Cyclin A/B RxL-IN-1 对 Cyclin A/B 表现出选择性结合亲和力，其 Cyclin A FP2 IC50 为 0.079 μM，而 Cyclin E FP2 IC50 为 0.958 μM[1]。

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

Cyclin A/B RxL-IN-1 相关抗体:
体内研究
(In Vivo)

Cyclin A/B RxL-IN-1 (Compound 34) (50-100 mg/kg，腹腔注射，每日一次，连续 14 天) 在 NCI-H1048 SCLC 移植瘤模型中诱导肿瘤生长抑制[1]。
Cyclin A/B RxL-IN-1 (100 mg/kg，腹腔注射，每日一次，连续 18 天) 在 NCI-H69 SCLC 移植瘤模型中表现出显著的抗肿瘤活性[1]。

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

Animal Model: NCI-H1048 cells (3 × 106 in 100 μL mixture of HITES media and Matrigel at 1:1 ratio) were subcutaneously implanted into the flanks of 6-8-week-old female BALB/c nude mice[1]
Dosage: 50, 100 mg/kg
Administration: i.p., once daily, 14 days
Result: Achieved tumor growth inhibition.
Showed no significant changes in body weight.
Animal Model: NCI-H69 cells (5 × 106 in 100 μL mixture of serum-free RPMI-1640 media and ECM gel at 1:1 ratio) were subcutaneously implanted into the flanks of 7-8-week-old female Nude mice[1]
Dosage: 100 mg/kg
Administration: i.p., once daily, 18 days
Result: Achieved tumor growth inhibition.
分子量

972.93

Formula

C46H63Cl2F4N7O7
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

Cyclin A/B RxL-IN-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:

Cyclin A/B RxL-IN-13036231-62-3CDKCyclin dependent kinasesmall-cell lung cancerCyclin A/BRB1/E2F-dysregulated cancer cellsInhibitorinhibitorinhibit

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