CDK9 inhibitor 2CAS# 1263369-28-3 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1263369-28-3 | SDF | Download SDF |
| PubChem ID | 49855228 | Appearance | Powder |
| Formula | C23H25ClFN5 | M.Wt | 425.93 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 50 mg/mL (117.39 mM; Need ultrasonic) | ||
| Chemical Name | 4-N-[5-chloro-4-[6-[(3-fluorophenyl)methylamino]pyridin-2-yl]pyridin-2-yl]cyclohexane-1,4-diamine | ||
| SMILES | C1CC(CCC1N)NC2=NC=C(C(=C2)C3=NC(=CC=C3)NCC4=CC(=CC=C4)F)Cl | ||
| Standard InChIKey | XKHXPTSUVPZYDW-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C23H25ClFN5/c24-20-14-28-23(29-18-9-7-17(26)8-10-18)12-19(20)21-5-2-6-22(30-21)27-13-15-3-1-4-16(25)11-15/h1-6,11-12,14,17-18H,7-10,13,26H2,(H,27,30)(H,28,29) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.In Vitro:CDK9-IN-2 (200 nM) reduces the expression of MEPCE indicating that MEPCE is a pharmacodynamic (PD) marker for any CDK9 inhibitor. The expression of MCL1 protein is reduced 2 hours after treatment and is further reduced after 16 hour exposure to CDK9-IN-2 (500 nM)[1]. References: | |||||
CDK9 inhibitor 2 Dilution Calculator
CDK9 inhibitor 2 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3478 mL | 11.739 mL | 23.478 mL | 46.9561 mL | 58.6951 mL |
| 5 mM | 0.4696 mL | 2.3478 mL | 4.6956 mL | 9.3912 mL | 11.739 mL |
| 10 mM | 0.2348 mL | 1.1739 mL | 2.3478 mL | 4.6956 mL | 5.8695 mL |
| 50 mM | 0.047 mL | 0.2348 mL | 0.4696 mL | 0.9391 mL | 1.1739 mL |
| 100 mM | 0.0235 mL | 0.1174 mL | 0.2348 mL | 0.4696 mL | 0.587 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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A novel Cyclin-dependent kinase 9 inhibitor.
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Targeting CDK9 by wogonin and related natural flavones potentiates the anti-cancer efficacy of the Bcl-2 family inhibitor ABT-263.[Pubmed:24895203]
Int J Cancer. 2015 Feb 1;136(3):688-98.
Tumor initiation, progression and resistance to therapies are tightly associated with over-expression of anti-apoptotic proteins Bcl-2, Bcl-x(L), Bcl-w and Mcl-1. ABT-263 (Navitoclax), an orally bio-available small-molecule mimetic of the Bcl-2 homology domain 3, inhibits Bcl-2, Bcl-x(L), and Bcl-w and has shown anti-cancer effects mainly on lymphomas and lymphocytic leukemia. Despite promising results obtained from the clinical trials, the use of ABT-263 in patients is dose-limited due to causing thrombocytopenia via inhibition of Bcl-x(L) in platelets. ABT-199 specifically inhibits Bcl-2; however, its use is limited to tumors over-expressing only Bcl-2. Besides, many tumors resist treatment due to high levels of Mcl-1 expression or develop resistance via up-regulation of Mcl-1 during long-term exposure. These obstacles highlight the demand to improve the ABT-263-based therapy. In this study, we show that anti-cancer flavones, e.g., wogonin, baicalein, apigenin, chrysin and luteolin enhance ABT-263-induced apoptosis in different cancer cell lines and in primary AML and ALL cells by down-regulation of Mcl-1 expression. Importantly, wogonin does not enhance the toxicity of ABT-263 to proliferating normal T cells and thrombocytes. Wogonin also potentiates the lethality of ABT-263 in cancer cells which have acquired resistance to ABT-263. Furthermore, we show that combination of wogonin with ABT-263 promotes in vivo tumor regression in a human T-cell leukemia xenograft mouse model. Our study demonstrates that wogonin (and related flavones) reduce the effective dose of ABT-263 thereby possibly decreasing the risk of adverse side effects.
