Art. -Nr.: HY-126251

CDK9-IN-7

Name: CDK9-IN-7
Brand: MedChemExpress
SKU: HY-126251
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CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC₅₀=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.

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Reinheit : 98.05%
CAS. Nr.: 2369981-71-3
Formel: C₂₉H₃₇N₇O₂S
Molecular Weight:547.71

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CDK9-IN-7 Chemical Structure

CAS. Nr.: 2369981-71-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (9)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

CDK9/cyclinT1

11 nM (IC₅₀)

CDK4/cyclin D

148 nM (IC₅₀)

CDK6/cyclinD

145 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.45 μM Compound: 21e	Antiproliferative activity against human A549 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
CCRF-CEM	IC₅₀	>10 μM Compound: 21e	Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
HCC827	IC₅₀	1.071 μM Compound: 21e	Antiproliferative activity against human HCC827 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human HCC827 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
HeLa	IC₅₀	1.85 μM Compound: 21e	Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
Hep 3B2	IC₅₀	5.61 μM Compound: 21e	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
HepG2	IC₅₀	3.861 μM Compound: 21e	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
Jurkat	IC₅₀	3.427 μM Compound: 21e	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
MCF7	IC₅₀	1.739 μM Compound: 21e	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
MDA-MB-231	IC₅₀	3.045 μM Compound: 21e	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
NCI-H1299	IC₅₀	0.203 μM Compound: 21e	Antiproliferative activity against human H1299 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human H1299 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
NCI-H1975	IC₅₀	0.837 μM Compound: 21e	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
PC-9	IC₅₀	0.947 μM Compound: 21e	Antiproliferative activity against human PC9 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human PC9 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
SiHa	IC₅₀	1.809 μM Compound: 21e	Antiproliferative activity against human SiHa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human SiHa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]
U-937	IC₅₀	1.988 μM Compound: 21e	Antiproliferative activity against human U937 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human U937 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 31376566]

In Vitro

CDK9-IN-7 displays exceptional potency against NSCLC cell lines, especial A549 and H1299 with IC₅₀ values less than 0.5 µM. In the drug-resistant NSCLC cell line H1975, CDK9-IN-7 also exhibits good inhibition potency with an IC₅₀ value of 0.837 µM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Chemical Information

CAS. Nr. 2369981-71-3
Appearance Solid
Molecular Weight 547.71
Formel C₂₉H₃₇N₇O₂S
Color Light yellow to yellow
SMILES

O=C(N(C)C)C1=CC2=CN=C(NC3=CC=C(NC(CCCCCCCN=C=S)=O)C=C3)N=C2N1C4CCCC4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 62.5 mg/mL (114.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8258 mL

9.1289 mL

18.2578 mL

5 mM

0.3652 mL

1.8258 mL

3.6516 mL

10 mM

0.1826 mL

0.9129 mL

1.8258 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

All Cell Biology Signal Pathway Related Animals and Diseases

Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang X, et al. Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer. Eur J Med Chem. 2019 Jul 25;181:111535. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8258 mL	9.1289 mL	18.2578 mL	45.6446 mL
	5 mM	0.3652 mL	1.8258 mL	3.6516 mL	9.1289 mL
	10 mM	0.1826 mL	0.9129 mL	1.8258 mL	4.5645 mL
	15 mM	0.1217 mL	0.6086 mL	1.2172 mL	3.0430 mL
	20 mM	0.0913 mL	0.4564 mL	0.9129 mL	2.2822 mL
	25 mM	0.0730 mL	0.3652 mL	0.7303 mL	1.8258 mL
	30 mM	0.0609 mL	0.3043 mL	0.6086 mL	1.5215 mL
	40 mM	0.0456 mL	0.2282 mL	0.4564 mL	1.1411 mL
	50 mM	0.0365 mL	0.1826 mL	0.3652 mL	0.9129 mL
	60 mM	0.0304 mL	0.1521 mL	0.3043 mL	0.7607 mL
	80 mM	0.0228 mL	0.1141 mL	0.2282 mL	0.5706 mL
	100 mM	0.0183 mL	0.0913 mL	0.1826 mL	0.4564 mL

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CDK9-IN-7

Alle CDK Isoform-spezifische Produkte anzeigen