2. PROTAC Cell Cycle/DNA Damage Apoptosis Epigenetics
  3. PROTACs CDK Caspase PARP Apoptosis
  4. dCDK9-202

dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015)).

For research use only. We do not sell to patients.

dCDK9-202

dCDK9-202 Chemical Structure

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dCDK9-202 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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View All Isoforms
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

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Description

dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015))[1].

IC50 & Target[1]

CDK9

3.5 nM (DC50)

Caspase-3

 

Caspase-7

 

Cereblon

 

In Vitro

dCDK9-202 (10 nM, 0-24 h) treatment of TC-71 cells within 2 hours can significantly reduce the CDK9 protein level, and complete and nearly continuous degradation was achieved within 8 hours[1].
dCDK9-202 (0.1 nM-1 μM, 24 h) exhibitx nanomolar levels of proliferation inhibitory activity in 12 cancer cell lines derived from various tissues such as lung, liver, bone, and brain. For instance, in TC-71 cells, the IC₅₀ is 8.5 nM[1].
dCDK9-202 (10-50 nM, 24 h) activates Caspase-3/7, increases the level of cleaved PARP, and directly induces apoptosis of TC-71 cells[1].
dCDK9-202 (0.25-25 nM, 6 h) significantly reduces the phosphorylation of Ser2 in the CTD domain of RNA polymerase II (p-Rpb1 Ser2) and downregulates a variety of short half-life proteins that are regulated by CDK9 and are closely related to cancer occurrence in TC-71 cells[1].

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

dCDK9-202 Related Antibodies

Western Blot Analysis[1]

Cell Line: TC-71 cells
Concentration: 10 and 50 nM
Incubation Time: 24 h
Result: Activated Caspase-3/7, increased the level of cleaved PARP.

Western Blot Analysis[1]

Cell Line: TC-71 cells
Concentration: 0.25, 2.5 and 25 nM
Incubation Time: 6 h
Result: Significantly reduced the phosphorylation of Ser2 in the CTD domain of RNA polymerase II (p-Rpb1 Ser2).
Strongly down-regulated a variety of short half-life proteins that are regulated by CDK9 and are closely related to cancer occurrence, such as MYC, MCL1, BCL-xL, etc.
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-t CL Vss
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 (10 mg/kg, i.v., once every other days for 7 doses) significantly inhibits the tumor volume and weight in the mouse xenograft tumor model established in the TC-71 cell line[1].

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

Animal Model: TC-71 cells xenografts model established in NCG mice (female, 6-8 weeks)[1]
Dosage: 10 mg/kg
Administration: Intravenous injection (i.v.), once every other days for 7 doses
Result: Significantly inhibited the tumor volume and weight.
Effectively reduced the level of CDK9 protein in tumor tissues after a single administration 2 hours later.
Did not show any weight loss or other obvious signs of toxicity in mice.
Molecular Weight

803.99

Formula

C40H49N7O7S2
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2438 mL 6.2190 mL 12.4380 mL
5 mM 0.2488 mL 1.2438 mL 2.4876 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

dCDK9-202PROTACsCDKCaspasePARPApoptosisCyclin dependent kinasepoly ADP ribose polymerase PROTACCDK9 degraderTC-71 cell linein vivo antitumor activitykinase selectivitytranscriptional addictionInhibitorinhibitorinhibit

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