Q901 hydrochloride
Based on 1 Customer Validation
Q901 hydrochloride (CDK7-IN-21 hydrochloride) is a selective covalent ATP-competitive CDK7 inhibitor with an IC50 value of 10 nM against human CDK7. Q901 hydrochloride 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 hydrochloride sensitizes tumors to topoisomerase I inhibitors and TOP1 inhibitor-based antibody-drug conjugates. Q901 hydrochloride 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 hydrochloride can be used for research on cancers such as ovarian cancer and lung cancer.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- 화학식: C33H37ClFN9O2
- 분자량:646.16
-
보관:
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]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- Protocol
- 순도&문서
- References
-
Help & FAQs
Biological Activity
제품 설명
|
CDK7 10 nM (IC50) |
Top1 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
95 nM
|
Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction by CellTiter-Glo luminescence after 72 hrs incubation.
Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction by CellTiter-Glo luminescence after 72 hrs incubation.
|
42814835 |
| MCF7 | IC50 |
16 nM
|
Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction by CellTiter-Glo luminescence after 96 hrs incubation.
Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction by CellTiter-Glo luminescence after 96 hrs incubation.
|
42814835 |
| MCF7 | IC50 |
5 nM
|
Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction by CellTiter-Glo luminescence after 120 hrs incubation.
Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction by CellTiter-Glo luminescence after 120 hrs incubation.
|
42814835 |
| HCT-116 | IC50 |
8.4 nM
|
Antiproliferative activity against human HCT116 colon cancer cells assessed as viability reduction by CellTiter-Glo after 72 hrs incubation.
Antiproliferative activity against human HCT116 colon cancer cells assessed as viability reduction by CellTiter-Glo after 72 hrs incubation.
|
42814835 |
| NCI-H292 | IC50 |
12 nM
|
Antiproliferative activity against human H292 lung cancer cells assessed as viability reduction by CellTiter-Glo after 72 hrs incubation.
Antiproliferative activity against human H292 lung cancer cells assessed as viability reduction by CellTiter-Glo after 72 hrs incubation.
|
42814835 |
In Vitro
Q901 (72-120 h) hydrochloride potently inhibits MCF-7 proliferation, with IC50 values of 95, 16, and 5 nM at 72, 96, and 120 h, respectively[3].
Q901 (100 nM; 1-24 h) hydrochloride reduces promoter-proximal RNAPII and traps CDK7 at promoters in MCF-7 cells[3].
Q901 (100 nM; 1-24 h) hydrochloride decreases promoter occupancy of MYC and E2F1 and reduces E2F1 expression in MCF-7 cells[3].
Q901 (100 nM; 4-24 h) hydrochloride impairs enhancer activity in MCF-7 cells but has no strong preferential effect on super-enhancer targets[3].
Q901 (10-1000 nM; 24-72 h) hydrochloride induces DNA damage and increases γH2AX expression in MCF-7 cells[3].
Q901 (100 nM; 30 min-24 h) hydrochloride stabilizes TOP1-DPC and inhibits DDR gene expression in MCF-7 cells[3].
Q901 (72 h) hydrochloride enhances the antiproliferative activity of Topotecan (TPT) (HY-13768) in H82, DMS53, and H446 SCLC cells[3].
Q901 (72 h) hydrochloride sensitizes HCT116 cells to T-DXd (HY-138298A) in vitro, with an IC50 of 8.4 nM for Q901[3].
Q901 (72 h) hydrochloride enhances the antiproliferative activity of Sacituzumab govitecan (SG) (HY-132254) in H292 cells, with an IC50 of 12 nM for Q901[3].
Q901 (100 μM; 72 h) hydrochloride inhibits the viability of H82, A2780, and MCF7 cells within 72 h in a dilution series starting at 100 μM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF-7 cells
-
Concentration:10, 100, 1000 nM
-
Incubation Time:24, 48, 72 h
-
Result:Increased γH2AX levels over time in a dose-dependent manner.
Pronounced P-H2AX induction was observed at 48 h with 1000 nM and at 72 h with 1000 nM.
-
Cell Line:A2780 cells
-
Concentration:6 nM
-
Incubation Time:4 h (exposure); washout at 0, 4, 24, and 48 h
-
Result:Free CDK7 levels were analyzed by immunoblotting at 0, 4, 24, and 48 h after washout.
CDK7 engagement was observed.
In Vivo
Q901 (3-10 mg/kg; i.p.; once daily) hydrochloride inhibits H292 xenograft tumor growth and enhances SG-induced tumor growth inhibition[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude[3]
-
Dosage:10 mg/kg
-
Administration:i.p.; once daily
-
Result:On day 28, 81% tumor growth inhibition was achieved; 102% tumor growth inhibition was achieved in the T-DXd-containing arm.
Tumors resumed growth by ∼11 days after dosing ended, whereas the T-DXd-containing arm maintained tumor suppression throughout the study.
-
Animal Model:BALB/c nude[3]
-
Dosage:10 mg/kg
-
Administration:i.p.; once daily
-
Result:By day 28, 80% tumor growth inhibition was achieved; 90% tumor growth inhibition was achieved in the SG-containing arm.
Sustained tumor growth inhibition was maintained throughout the study period, with slightly higher efficacy in the SG-containing arm.
-
Animal Model:BALB/c nude[3]
-
Dosage:3 mg/kg
-
Administration:i.p.; once daily
-
Result:By day 28, 61% tumor growth inhibition was achieved; 92% tumor growth inhibition was achieved in the SG-containing arm.
Sustained tumor growth inhibition was maintained throughout the study period.
Chemical Information
-
분자량 646.16
-
화학식 C33H37ClFN9O2
-
SMILES
C=C(C(NC1=CC2=C(C(C3=C(CNC4=NC(NC[C@@H]5[C@@H](O)CNCC5)=NC6=C(C(C)C)C=NN46)C=CC=C3)=NC=C2)C=C1)=O)F.Cl
-
Synonyms
CDK7-IN-21 hydrochloride
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
용액&용해도
In Vitro:
DMSO : 100 mg/mL (154.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
순도&문서
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5476 mL | 7.7380 mL | 15.4760 mL | 38.6901 mL |
| 5 mM | 0.3095 mL | 1.5476 mL | 3.0952 mL | 7.7380 mL | |
| 10 mM | 0.1548 mL | 0.7738 mL | 1.5476 mL | 3.8690 mL | |
| 15 mM | 0.1032 mL | 0.5159 mL | 1.0317 mL | 2.5793 mL | |
| 20 mM | 0.0774 mL | 0.3869 mL | 0.7738 mL | 1.9345 mL | |
| 25 mM | 0.0619 mL | 0.3095 mL | 0.6190 mL | 1.5476 mL | |
| 30 mM | 0.0516 mL | 0.2579 mL | 0.5159 mL | 1.2897 mL | |
| 40 mM | 0.0387 mL | 0.1935 mL | 0.3869 mL | 0.9673 mL | |
| 50 mM | 0.0310 mL | 0.1548 mL | 0.3095 mL | 0.7738 mL | |
| 60 mM | 0.0258 mL | 0.1290 mL | 0.2579 mL | 0.6448 mL | |
| 80 mM | 0.0193 mL | 0.0967 mL | 0.1935 mL | 0.4836 mL | |
| 100 mM | 0.0155 mL | 0.0774 mL | 0.1548 mL | 0.3869 mL |
Q901 hydrochloride Related Classifications
HY-153278B Related Classifications
Powered by Bioz