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

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.

For research use only. We do not sell to patients.

CTX-439

CTX-439 Chemical Structure

CAS No. : 2377487-13-1

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Description

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].

In Vitro

CTX-439 (0-10 μM; 6-72 h) inhibits the proliferation of SUM149PT cells with an IC50 of 100.5 nM, induces DNA damage and apoptosis, and downregulates the expression of DNA damage repair genes by inhibiting CDK12 activity[1].
CTX-439 (0-1 μM; 0-24 h) downregulates MCL1 protein levels in SUM149PT and OV90 cells[1].
CTX-439 (100-800 nM; 4-8 h) synergizes with the BCL-2/BCL-xL inhibitor AZD4320 (HY-112416) to rapidly induce apoptosis in SUM149PT and OV90 cells[1].

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

CTX-439 Related Antibodies
In Vivo

CTX-439 (7.5-30 mg/kg; p.o.; twice weekly; 15 days) inhibits the growth of SUM149PT breast cancer xenografts in nude mice in a dose-dependent manner[1].

MedChemExpress (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.
Molecular Weight

671.69

Formula

C30H32F3N9O4S
CAS No.
SMILES

O=C(CCC)N(C1=CN=C(C2=CN=C(OC)N=C2)C=N1)[C@@H]3CC[C@@H](NC4=NC(C5=CC(S(C)(=O)=O)=CN=C5)=C(C(F)(F)F)C=N4)CC3
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CTX-439 Related Classifications

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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:

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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