2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs CDK Apoptosis
  4. CXJ2080

CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC50 of 0.88 nM. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia.
(Pink: CDK7 ligand (HY-183071); Blue: VHL ligand (HY-170348); Black: linker).

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

CXJ2080

CXJ2080 Chemical Structure

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CXJ2080 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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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

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Description

CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC50 of 0.88 nM. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia[1]. (Pink: CDK7 ligand (HY-183071); Blue: VHL ligand (HY-170348); Black: linker).

IC50 & Target[1]

CDK7

 

In Vitro

CXJ2080 (0.5-200 nM; 6 h) potently degrades CDK7 in MV4-11 acute myeloid leukemia cells with a DC50 of 0.88 nM and >98% maximum degradation efficiency[1].
CXJ2080 (72 h) potently inhibits the proliferation of RS4;11 acute lymphoblastic leukemia cells (IC50 = 17.29 nM) and MV4-11 acute myeloid leukemia cells (IC50 = 4.31 nM)[1].
CXJ2080 (72 h) inhibits the proliferation of primary acute myeloid leukemia patient-derived cell samples[1].
CXJ2080 (100 nM; 4 h pretreatment) induces sustained CDK7 degradation in MV4-11 acute myeloid leukemia cells, with suppression maintained for 48 h post-washout[1].
CXJ2080 (5-100 nM; 8 h) induces dose-dependent CDK7 degradation, p53 accumulation, Myc downregulation, and a biphasic p21 protein response in MV4-11 acute myeloid leukemia cells[1].
CXJ2080 (5-100 nM; 12 h) induces dose-dependent cell cycle arrest in MV4-11 acute myeloid leukemia cells, with increased SubG1 phase accumulation at higher concentrations[1].
CXJ2080 (5-100 nM; 48 h) induces dose-dependent apoptosis in MV4-11 acute myeloid leukemia cells[1].
CXJ2080 (5-100 nM; 24 h) significantly reduces CD117 (c-KIT) stemness marker expression in MV4-11 acute myeloid leukemia cells[1].

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

CXJ2080 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 100 nM
Incubation Time: 4 h
Result: Maintained CDK7 degradation for 48 h post-washout.

Western Blot Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 5 nM; 20 nM; 100 nM
Incubation Time: 8 h
Result: Degraded CDK7 in a dose-dependent manner.
Induced accumulation of p53 protein.
Downregulated Myc protein.
Caused a biphasic response in p21 protein levels (upregulated at low concentrations, downregulated at high concentrations).

Cell Cycle Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 5 nM; 20 nM; 100 nM
Incubation Time: 12 h
Result: Induced cell cycle arrest in a dose-dependent manner.
Increased accumulation of cells in the SubG1 phase at higher concentrations.

Apoptosis Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 5 nM; 20 nM; 100 nM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner.
Showed a higher proportion of apoptotic cells observed at higher concentrations.
Exhibited more potent apoptotic effects than TZ1104.
Parmacokinetics
Species Dose Route AUC0-t F T1/2
Mice[1] 10 mg/kg i.p. 1014 ng·h/mL 81.6 % /
Mice[1] 10 mg/kg i.v. / / 2.5 h
Mice[1] 10 mg/kg i.v. / / 2.5 h
In Vivo

CXJ2080 (20-50 mg/kg; i.v.; every other day; 2 weeks) administered at 50 mg/kg every other day via intravenous injection achieves potent tumor growth inhibition with selective CDK7 degradation in RS4;11 xenograft tumors, while sparing PBMCs[1].
CXJ2080 (20-50 mg/kg; i.v.; every other day; 3 weeks) administered at 50 mg/kg every other day via intravenous injection achieves potent tumor growth inhibition with selective CDK7 degradation in MV4-11 xenograft tumors, while sparing PBMCs and maintaining normal platelet parameters[1].
CXJ2080 (20 mg/kg; i.v.; every other day; 21 days) administered at 20 mg/kg every other day via intravenous injection significantly improves survival in mice with disseminated Molm13 acute myeloid leukemia[1].

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

Animal Model: Nu/Nu (female; 6-8 weeks old; implanted subcutaneously in
the right flank with 5 × 106 RS4;11 cells for a RS4;11 subcutaneous xenograft model)[1]
Dosage: 20 mg/kg; 50 mg/kg
Administration: i.v.; every other day; 2 weeks
Result: Resulted in tumor weights similar to vehicle controls at 20 mg/kg.
Significantly reduced tumor weights relative to vehicle controls at 50 mg/kg.
Achieved robust CDK7 degradation in tumor tissues at 50 mg/kg.
Caused no significant reduction in CDK7 levels in PBMCs at 50 mg/kg.
Animal Model: Nu/Nu (female; 6-8 weeks old; implanted subcutaneously in
the right flank with 5 × 106 MV4-11cells for a MV4-11 subcutaneous xenograft model)[1]
Dosage: 20 mg/kg; 50 mg/kg
Administration: i.v.; every other day; 3 weeks
Result: Resulted in tumor weights similar to vehicle controls at 20 mg/kg.
Significantly reduced tumor weights relative to vehicle controls at 50 mg/kg.
Achieved robust CDK7 degradation in tumor tissues at 50 mg/kg.
Caused no significant reduction in CDK7 levels in PBMCs at 50 mg/kg.
Maintained stable platelet counts, platelet-large cell ratio (P-LCR), and plateletcrit (PCT) throughout the treatment period at 50 mg/kg.
Animal Model: NOD scid gamma (NSG) (female; 6-8 weeks old; inoculated intravenously with 2 × 104
Molm13 cells via the tail vein for a Molm13 disseminated xenograft model)[1]
Dosage: 20 mg/kg
Administration: i.v.; every other day; 21 days
Result: Significantly extended the survival of Molm13 tumor-bearing mice relative to vehicle controls.
Maintained a low leukemia burden in spleens of two surviving mice at the experimental endpoint.
Molecular Weight

1030.74

Formula

C51H68ClN11O6S2
SMILES

O=C([C@H]1N(C([C@@H](N2N=NC(CCCCCCC(N[C@H]3CC[C@H](NC4=NC=C(Cl)C(NC5=CC=CC=C5S(=O)(C(C)C)=O)=N4)CC3)=O)=C2)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
Shipping

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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CXJ2080 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:

CXJ2080CXJ 2080CXJ-2080PROTACsCDKApoptosisCyclin dependent kinaseRS4;11 acute lymphoblastic leukemia cellsRNA polymerase II CTD Ser5p53-p21 axisubiquitin-proteasomeCDK2 Thr160MV4-11 acute myeloid leukemia cellsVHL E3 ligaseCDK1 Thr161MYCCDK7Inhibitorinhibitorinhibit

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