dCDK9-202 |
Katalog-Nr.GC81512
One-Click Copy Product Info
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dCDK9-202 is a CDK9 PROTAC degrader with a DC50 of 3.5 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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].
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].
References:
[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.
| Cas No. | SDF | ||
| Formula | C40H49N7O7S2 | M.Wt | 803.99 |
| Löslichkeit | DMSO: 100 mg/mL (124.38 mM; Need ultrasonic) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.2438 mL | 6.219 mL | 12.438 mL |
| 5 mM | 248.8 μL | 1.2438 mL | 2.4876 mL |
| 10 mM | 124.4 μL | 621.9 μL | 1.2438 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)