2766124-39-2
Chemical Structure
Q901
Synonym(s): CDK7-IN-21
- CAS No.: 2766124-39-2
- Formula:C33H36FN9O2
- Molecular Weight:609.70
IUPAC Name: 2-fluoro-N-(1-(2-(((2-((((3R,4R)-3-hydroxypiperidin-4-yl)methyl)amino)-8-isopropylpyrazolo[1,5-a][1,3,5]triazin-4-yl)amino)methyl)phenyl)isoquinolin-6-yl)acrylamide
InChIKey: PDKSTEKFCWNJFC-LXFBAYGMSA-N
SMILES: C=C(F)C(NC(C=C1)=CC2=C1C(C(C=CC=C3)=C3CNC(N4N=C5)=NC(NC[C@@H]6[C@H](CNCC6)O)=NC4=C5C(C)C)=NC=C2)=O
Biological Activity: Q901 (CDK7-IN-21) is a selective covalent ATP-competitive CDK7 inhibitor with an IC50 value of 10 nM against human CDK7. Q901 inhibits MYC/E2F-dependent oncogenic transcription, the RNAPII transition from initiation to elongation, and DNA damage repair, stabilizes TOP1-DNA protein crosslinks, and induces DNA damage. Q901 sensitizes tumors to topoisomerase I inhibitors and TOP1 inhibitor-based antibody-drug conjugates. Q901 shows additive or synergistic tumor growth inhibition in solid tumor models in combination with PARP inhibitors, SERDs, ER PROTAC degraders, or anti-PD-1 antibodies. Q901 can be used for research on cancers such as ovarian cancer and lung cancer[1][2][3][4].
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Q901 | Q901 (CDK7-IN-21) is a selective covalent ATP-competitive CDK7 inhibitor with an IC50 value of 10 nM against human CDK7. Q901 inhibits MYC/E2F-dependent oncogenic transcription, the RNAPII transition from initiation to elongation, and DNA damage repair, stabilizes TOP1-DNA protein crosslinks, and induces DNA damage. Q901 sensitizes tumors to topoisomerase I inhibitors and TOP1 inhibitor-based antibody-drug conjugates. Q901 shows additive or synergistic tumor growth inhibition in solid tumor models in combination with PARP inhibitors, SERDs, ER PROTAC degraders, or anti-PD-1 antibodies. Q901 can be used for research on cancers such as ovarian cancer and lung cancer. | |||||||||||||||||||||
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References
- [1]. Jung H, et al. Sensitizing tumor response to topoisomerase I antibody drug conjugate by selective CDK7 inhibition. bioRxiv [Preprint]. 2025 Nov 25:2025.11.23.690049. doi: 10.1101/2025.11.23.690049. Update in: Sci Adv. 2026 Oct 2;12(40):eaeb4023. [Content Brief]
- [2]. Donghoon Yu, et al. Abstract 5977: Evaluation of the potential combination regimens for q901, a clinical stage selective cdk7 inhibitor, as a DNA damage repair inhibitor. Cancer Res 1 April 2023; 83 (7_Supplement): 5977.
- [3]. Jung H, et al. Sensitizing tumor response to topoisomerase I antibody-drug conjugate by selective CDK7 inhibition. Science advances. 2026 Oct 02;12(40):eaeb4023.
