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)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C49H66ClN9O7S2
- 分子量:992.69
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
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Cell Line:MV4-11 cells
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Concentration:0.1 nM; 1 nM; 10 nM
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Incubation Time:6 h
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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.
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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
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Administration:i.p.; twice daily; 26 days
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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.
化学情報
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分子量 992.69
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分子式 C49H66ClN9O7S2
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TZ1104 関連分類
HY-183073 関連分類
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