TZ1104
TZ1104 is a PROTAC-based CDK7 degrader, with a DC50 of 0.88 nM. TZ1104 forms a ternary complex with VHL E3 ligase and CDK7 to trigger proteasome-dependent CDK7 degradation, destabilizing the CDK7-cyclin H-MAT1 complex. TZ1104 suppresses phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. TZ1104 activates the p53-p21 axis and suppresses oncogenic Myc signaling. TZ1104 induces cell cycle arrest, apoptosis, and differentiation of acute leukemia cells. TZ1104 can be used for the research of acute leukemia.
(Pink: CDK7 ligand (HY-183071); Blue: VHL ligand (HY-112078); Black: linker (HY-W108876)).
For research use only. We do not sell to patients.
- Formula: C49H66ClN9O7S2
- Molecular Weight:992.69
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
TZ1104 (0.1-nM μM; 6 h) emerges as a potent CDK7 degrader and achieves a half degradation concentration (DC50) of 4.92 nM and a maximum degradation (Dmax) of 98.87% in MV4-11 cells[1].
TZ1104 (72 h) shows potent and broad CDK7 degradation across various
acute leukemia cell lines, encompassing AML (Molm13, THP-1, HL60,
CESS) and ALL (RS4;11) models[1].
TZ1104 demonstrates significantly enhanced antiproliferative effects while maintaining minimal cytotoxicity in human peripheral blood mononuclear cells (PBMCs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MV4-11 cells
-
Concentration:0.1 nM; 1 nM; 10 nM
-
Incubation Time:6 h
-
Result:Emerged as a potent CDK7 degrader and achieved a half degradation concentration (DC50) of 4.92 nM and a maximum degradation (Dmax).
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 MV4-11 cells for a MV4-11 subcutaneous xenograft model)[1] -
Dosage:50 mg/kg
-
Administration:i.p.; twice daily; 26 days
-
Result:Reduced tumor weight relative to vehicle control.
Induced robust CDK7 degradation in tumor tissues.
Caused no significant CDK7 reduction in PBMCs.
Caused no observable body weight loss during treatment.
Chemical Information
-
Molecular Weight 992.69
-
Formula C49H66ClN9O7S2
-
SMILES
O=C(N[C@H]1CC[C@H](NC2=NC=C(Cl)C(NC3=CC=CC=C3S(=O)(C(C)C)=O)=N2)CC1)CCCCCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)=O
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz