KI-CDK9d-32
Based on 1 Customer Validation
KI-CDK9d-32 is a highly selective and potent CDK9 PROTAC degrader (DC50: 0.89 nM). KI-CDK9d-32 promotes the ubiquitination and degradation of CDK9. KI-CDK9d-32 inhibits the MYC pathway and disrupts nucleolar homeostasis. KI-CDK9d-32 exhibits anticancer activity against acute lymphoblastic leukemia and pancreatic cancer.
(Pink: CDK9 ligand (HY-153718); Blue: Cereblon ligand (HY-163233); Black: linker (HY-W011657)).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.03%
- CAS 番号: 3054009-82-1
- 分子式: C39H45N9O4
- 分子量:703.83
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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CDK9 0.89 nM (DC50) |
KI-CDK9d-32 (4 h) achieves near 100% maximal degradation of CDK9 and a DC50 of 0.89 nM in MOLT-4 cells[1].
KI-CDK9d-32 (15 nM; 2-8 h) induces a rapid and sustained downregulation of MYC mRNA expression in MOLT-4 cells[1].
KI-CDK9d-32 (50 nM; 4 h) leads to the most significant downregulation of CDK9 and MYC protein levels in MOLT-4 cells[2].
KI-CDK9d-32 shows 72 h IC50 values of 2.8 nM, 21.3 nM, and 52.9 nM in MOLT-4, PSN-1, and RH-4 cells, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 3054009-82-1
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性状 Solid
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分子量 703.83
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分子式 C39H45N9O4
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Color White to off-white
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SMILES
O=C(N[C@H]1C[C@H](NC2=CC(CCC)=NC3=CC=NN23)CC1)C4=CC=C(CN5CCN(C6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7)=O)C=C6)CC5)C=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (142.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.55 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.55 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Toure MA, et al. Targeted degradation of CDK9 potently disrupts the MYC-regulated network. Cell Chem Biol. 2025 Apr 17;32(4):542-555.e10. [Content Brief]
[2]. Yin J, et al. Beyond Inhibition: Recent Advances of Heterobifunctional Molecules Targeting CDK9. J Med Chem. 2025 Nov 13;68(21):22095-22115. [Content Brief]
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 | 1.4208 mL | 7.1040 mL | 14.2080 mL | 35.5199 mL |
| 5 mM | 0.2842 mL | 1.4208 mL | 2.8416 mL | 7.1040 mL | |
| 10 mM | 0.1421 mL | 0.7104 mL | 1.4208 mL | 3.5520 mL | |
| 15 mM | 0.0947 mL | 0.4736 mL | 0.9472 mL | 2.3680 mL | |
| 20 mM | 0.0710 mL | 0.3552 mL | 0.7104 mL | 1.7760 mL | |
| 25 mM | 0.0568 mL | 0.2842 mL | 0.5683 mL | 1.4208 mL | |
| 30 mM | 0.0474 mL | 0.2368 mL | 0.4736 mL | 1.1840 mL | |
| 40 mM | 0.0355 mL | 0.1776 mL | 0.3552 mL | 0.8880 mL | |
| 50 mM | 0.0284 mL | 0.1421 mL | 0.2842 mL | 0.7104 mL | |
| 60 mM | 0.0237 mL | 0.1184 mL | 0.2368 mL | 0.5920 mL | |
| 80 mM | 0.0178 mL | 0.0888 mL | 0.1776 mL | 0.4440 mL | |
| 100 mM | 0.0142 mL | 0.0710 mL | 0.1421 mL | 0.3552 mL |
KI-CDK9d-32 関連分類
HY-173523 関連分類
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