2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. CTX-439

CTX-439 是一种具有口服活性的 ATP 竞争性小分子 CDK12 和 CDK13 抑制剂，对 CDK12 的 IC50 为 3.1 nM，Kd 为 0.38 nM，CDK13 的 IC50 为 9.2 nM。CTX-439 可诱导肿瘤细胞 DNA 损伤与凋亡 (apoptosis)。CTX-439 可用于乳腺癌、卵巢癌的研究。

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CTX-439

CTX-439 Chemical Structure

CAS No. : 2377487-13-1

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CTX-439 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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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

CTX-439 is an orally active, ATP-competitive small-molecule inhibitor of CDK12 and CDK13, with an IC50 of 3.1 nM and a Kd of 0.38 nM against CDK12, and an IC50 of 9.2 nM against CDK13. CTX-439 induces DNA damage and apoptosis in tumor cells. CTX-439 is applicable for the research of breast cancer and ovarian cancer[1].

体外研究
(In Vitro)

CTX-439 (0-10 μM; 6-72 h) 可抑制 SUM149PT 细胞增殖，其 IC50 为 100.5 nM，还可诱导 DNA 损伤与细胞凋亡，并通过抑制 CDK12 活性下调 DNA 损伤修复基因的表达[1]。
CTX-439 (0-1 μM; 0-24 h) 可下调 SUM149PT 和 OV90 细胞中的 MCL1 蛋白水平[1]。
CTX-439 (100-800 nM; 4-8 h) 可与 BCL-2/BCL-xL 抑制剂 AZD4320 (HY-112416) 产生协同作用，在 SUM149PT 和 OV90 细胞中快速诱导细胞凋亡[1]。

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

CTX-439 相关抗体:
体内研究
(In Vivo)

CTX-439 (7.5-30 mg/kg；灌胃；每周 2 次；15 天) 可呈剂量依赖性抑制裸鼠体内 SUM149PT 乳腺癌异种移植物的生长[1]。

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

Animal Model: BALB/cA Jcl-nu/nu (6-week-old, nude, subcutaneous injection of 3 × 106 SUM149PT cells)[1]
Dosage: 7.5 mg/kg; 15 mg/kg; 30 mg/kg
Administration: i.g.; twice weekly; 15 days
Result: Significantly suppressed tumor growth.
Caused tumor regression.
Did not cause significant weight loss at any dose.
Animal Model: BALB/cA Jcl-nu/nu (6-week-old, nude, subcutaneous injection of 3 × 106 SUM149PT cells)[1]
Dosage: 7.5 mg/kg
Administration: i.g.; twice weekly; 15 days
Result: Significantly suppressed tumor growth relative to vehicle, with final tumor volumes lower than vehicle but higher than combination treatment.
Downregulated MCL1 protein levels, reduced CDK12 S423 phosphorylation, and induced cleaved PARP and cleaved Caspase-3 levels in tumor tissue.
Did not cause significant weight loss.
分子量

671.69

Formula

C30H32F3N9O4S
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

CTX-439 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

CTX-4392377487-13-1CTX439CTX 439CDKApoptosisCyclin dependent kinaseBCL-2/BCL-xL inhibitorsMCL1CDK12OV90 cellsRNA polymerase II C-terminal domainbreast cancer patient-derived xenograft modelsCDK13ovarian cancerSUM149PT cellsbreast cancerInhibitorinhibitorinhibit

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HY-182312
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