Art. -Nr.: HY-178861

dCDK9-202

Name: dCDK9-202
Brand: MedChemExpress
SKU: HY-178861
Price: 250.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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dCDK9-202 is a CDK9 PROTAC degrader with a DC₅₀ of 3.5 nM. dCDK9-202 induces CDK9 degradation via the ubiquitin-proteasome system. dCDK9-202 inhibits the growth of cancer cells in vitro and suppresses tumor growth in mouse xenograft models. dCDK9-202 is applicable for cancer-related research.
(Pink: CDK9 ligand (HY-10008); Blue: Cereblon ligand (HY-W248665); Black: linker (HY-N8015)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.74%
Formel: C₄₀H₄₉N₇O₇S₂
Molecular Weight:803.99

Speicherung:

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

dCDK9-202 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

dCDK9-202 is a CDK9 PROTAC degrader with a DC₅₀ of 3.5 nM. dCDK9-202 induces CDK9 degradation via the ubiquitin-proteasome system. dCDK9-202 inhibits the growth of cancer cells in vitro and suppresses tumor growth in mouse xenograft models. dCDK9-202 is applicable for cancer-related research^[1]. (Pink: CDK9 ligand (HY-10008); Blue: Cereblon ligand (HY-W248665); Black: linker (HY-N8015)).

IC₅₀ & Target

^[1]

CDK9

3.5 nM (DC₅₀)

Caspase-3

Caspase-7

CDK4

CDK5

CDK6

CDK8

CDK11

IKZF3

Bcl-xL

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Alle PARP Isoform-spezifische Produkte anzeigen :

Alle IKZF Family Isoform-spezifische Produkte anzeigen :

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
SK-UT-1	DC₅₀	<10 nM	CDK9 degradation in human SKUT1 uterine leiomyosarcoma cells measured by Western blotting after 6 h treatment. CDK9 degradation in human SKUT1 uterine leiomyosarcoma cells measured by Western blotting after 6 h treatment.	41066447
A-375	IC₅₀	83.3 nM	Antiproliferative activity against human A-375 melanoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human A-375 melanoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	41066447
MES-SA	IC₅₀	85.3 nM	Antiproliferative activity against human MES-SA uterine sarcoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human MES-SA uterine sarcoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	41066447
MDA-MB-231	IC₅₀	79.6 nM	Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	41066447
A673	IC₅₀	75.4 nM	Antiproliferative activity against human A-673 Ewing sarcoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human A-673 Ewing sarcoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	41066447
NCI-H226	IC₅₀	57.0 nM	Antiproliferative activity against human NCI-H226 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human NCI-H226 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	41066447
NALM-6	IC₅₀	23.4 nM	Antiproliferative activity against human NALM6 B cell acute lymphoblastic leukemia cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human NALM6 B cell acute lymphoblastic leukemia cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	41066447
SJSA-1	IC₅₀	174.2 nM	Antiproliferative activity against human SJSA-1 osteosarcoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human SJSA-1 osteosarcoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	41066447
U-87MG ATCC	IC₅₀	33.9 nM	Antiproliferative activity against human U87 glioblastoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human U87 glioblastoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	41066447
SK-UT-1	IC₅₀	106.3 nM	Antiproliferative activity against human SKUT1 uterine leiomyosarcoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human SKUT1 uterine leiomyosarcoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	41066447
REH	IC₅₀	6.6 nM	Antiproliferative activity against human REH acute lymphocytic leukemia cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human REH acute lymphocytic leukemia cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	41066447

In Vitro

dCDK9-202 (compound 14) (0.25-25 nM; 2-24 h) potently and selectively degrades CDK9 in TC-71 Ewing sarcoma cells via a proteasome-dependent CRBN-mediated mechanism, with a DC₅₀ of 3.5 nM, and achieves nearly complete degradation within 8 h at a concentration of 10 nM^[1].
dCDK9-202 (0.25-25 nM; 6 h) potently degrades CDK9 in U87 glioblastoma cells, SKUT1 uterine leiomyosarcoma cells and RH5 rhabdomyosarcoma cells, with a DC₅₀ value of less than 10 nM^[1].
dCDK9-202 (72 h) potently inhibits the growth of various human cancer cell lines derived from different tissues, with IC₅₀ values ranging from 2.4 nM (RH5 rhabdomyosarcoma) to 174.2 nM (SJSA-1 osteosarcoma)^[1].
dCDK9-202 (10 nM; 0-24 h) selectively degrades CDK9 in TC-71 Ewing sarcoma cells within 8 h, without inducing acute off-target degradation of IKZF1/3 or other CDK family members^[1].
dCDK9-202 (0.25-25 nM; 6-8 h) impairs Pol2 activity and disrupts the oncogenic transcriptome in TC-71 Ewing sarcoma cells, reduces Pol2 phosphorylation levels, inhibits key oncoproteins and anti-apoptotic proteins, and suppresses pro-tumor signaling pathways^[1].
dCDK9-202 (10-50 nM; 24 h) inhibits DNA replication and induces apoptosis in TC-71 Ewing sarcoma cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

TC-71 Ewing sarcoma cells
Concentration:

10 nM (time-course)
0.25 nM, 2.5 nM, 25 nM (6 h treatment)
20 nM (inhibitor pre-treatment)
Incubation Time:

2 h, 4 h, 8 h, 12 h, 24 h (10 nM time-course)
6 h (0.25-25 nM treatment)
4 h (20 nM treatment, preceded by 2 h pre-treatment)
Result:

Achieved near-complete CDK9 degradation within 8 h of 10 nM treatment, with durable degradation maintained through 24 h.
Efficiently depleted CDK9 protein at concentrations as low as 0.25 nM after 6 h treatment.
Blocked CDK9 degradation by pre-treatment with 10 μM cyclin-dependent kinase inhibitor SNS032 (HY-10008), 10 μM immunomodulatory imide drug thalidomide, 5 μM (R)-MG132 (HY-13259C) proteasome inhibitor, or 2 μM NEDD8-activating enzyme inhibitor MLN4924 (HY-70062).

Western Blot Analysis^[1]

Cell Line:

U87 glioblastoma, SKUT1 uterine leiomyosarcoma, and RH5 rhabdomyosarcoma cells
Concentration:

0.25 nM, 2.5 nM, 25 nM
Incubation Time:

6 h
Result:

Significantly depleted endogenous CDK9 at all tested concentrations in U87, SKUT1, and RH5 cells, with DC₅₀ values below 10 nM in all three cell lines.

Western Blot Analysis^[1]

Cell Line:

TC-71 Ewing sarcoma cells
Concentration:

10, 50 nM
Incubation Time:

24 h
Result:

Inhibited DNA replication and induces apoptosis in TC-71 Ewing sarcoma cells, with near-complete CDK9 depletion and elevated apoptotic markers observed after 24 h treatment at 50 nM.

Western Blot Analysis^[1]

Cell Line:

TC-71 Ewing sarcoma cells
Concentration:

10 nM
Incubation Time:

0 h, 2 h, 4 h, 8 h, 12 h, 24 h
Result:

Induced selective degradation of CDK9 within 8 h, with no acute depletion of IKZF1/3.
Downregulated CDK4/5/6/8/11 and IKZF3 after 12 h, indicating a secondary effect.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	AUC_0-t	CL	V_ss
Mice^[1]	2 mg/kg	i.v.	0.3 h	280 ng/mL	116 ng·h/mL	312 mL/min/kg	7.1 L/kg

In Vivo

dCDK9-202 (compound 14) (10 mg/kg; i.v.; every other day for 7 doses; single dose) potently inhibits TC-71 Ewing sarcoma xenograft growth and reduces intratumoral CDK9 protein levels, without causing detectable toxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NCG (NOD/ShiLtJGpt-Prkdcem26Cd52Il2rgem26Cd22/Gpt) mice (female, 6 to 8 weeks old, subcutaneous xenograft model, One million TC-71 cells were mixed with 100 μL of PBS/Matrigel solution (1:1) and implanted subcutaneously into the dorsal flank of
recipient mice)^[1]
Dosage:

10 mg/kg
Administration:

i.v.; every other day for 7 doses; single dose (PD testing)
Result:

Significantly reduced TC-71 xenograft tumor volume and tumor weight over a 12-day treatment period.
Reduced intratumoral CDK9 protein levels within 2 hours following a single dose.
Reduced spleen CDK9 protein levels within 2 hours following a single dose, with levels returning by 6 hours.
Caused no body weight loss in treated mice.

Chemical Information

Appearance Solid
Molecular Weight 803.99
Formel C₄₀H₄₉N₇O₇S₂
Color White to off-white
SMILES

CC(C)(C1=CN=C(O1)CSC2=CN=C(S2)NC(C3CCN(CC3)C(CCCCCCCN4CC5=C(C4)C=C6C(N(C(C6=C5)=O)C7CCC(NC7=O)=O)=O)=O)=O)C
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 : 100 mg/mL (124.38 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

1.2438 mL

6.2190 mL

12.4380 mL

5 mM

0.2488 mL

1.2438 mL

2.4876 mL

10 mM

0.1244 mL

0.6219 mL

1.2438 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: ≥ 2.5 mg/mL (3.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Ma L, et al. Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong Antitumor Activity. Journal of medicinal chemistry. 2025 Oct 23;68(20):21172-21186. [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	1.2438 mL	6.2190 mL	12.4380 mL	31.0949 mL
	5 mM	0.2488 mL	1.2438 mL	2.4876 mL	6.2190 mL
	10 mM	0.1244 mL	0.6219 mL	1.2438 mL	3.1095 mL
	15 mM	0.0829 mL	0.4146 mL	0.8292 mL	2.0730 mL
	20 mM	0.0622 mL	0.3109 mL	0.6219 mL	1.5547 mL
	25 mM	0.0498 mL	0.2488 mL	0.4975 mL	1.2438 mL
	30 mM	0.0415 mL	0.2073 mL	0.4146 mL	1.0365 mL
	40 mM	0.0311 mL	0.1555 mL	0.3109 mL	0.7774 mL
	50 mM	0.0249 mL	0.1244 mL	0.2488 mL	0.6219 mL
	60 mM	0.0207 mL	0.1036 mL	0.2073 mL	0.5182 mL
	80 mM	0.0155 mL	0.0777 mL	0.1555 mL	0.3887 mL
	100 mM	0.0124 mL	0.0622 mL	0.1244 mL	0.3109 mL

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dCDK9-202

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Alle PARP Isoform-spezifische Produkte anzeigen

Alle IKZF Family Isoform-spezifische Produkte anzeigen

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen