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CDK9 inhibitor 2

Catalog No.GC17359

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CDK9 inhibitor 2 Chemical Structure

Cas No.: 1263369-28-3

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10mM (in 1mL DMSO)
$263.00
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5mg
$239.00
In stock
10mg
$309.00
In stock
50mg
$834.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

H929, A2058, A375, U87MG, and NCIH441 cell lines are treated with CDK9-IN-2 at 500 nM (high) or 200 nM (low) at different time points. Five cell lines are analyzed: NCI-H929, a multiple myeloma cell line; NCI-H441 , a lung papillary adenocarcinoma cell line; A375, a melanoma cell line; A2058, a melanoma cell line and U-87-MG, a glioblastoma cell line. Cell lines are grown in the medium recommended by ATCC and treated as follows: NCI-H929: 2 hours: DMSO, 200 nM CDK9-IN-2 or 500nM CDK9-IN-2. NCI-H441 and A375: 0 timepoint: Untreated, harvested when compound is added to the other plates. 2 hours: DMSO, 200 nM CDK9-IN-2 or 500 nM CDK9-IN-2 or 500 nM CKDI(7) (3 plates each, total 12 plates).8 hours: DMSO, 200 nM CDK9-IN-2 or 500 nM CDK9-IN-2 or 500 nM CKDI(7) (3 plates each, total 12 plates).16 hours: DMSO, 200 nM CDK9-IN-2 or 500 nM CDK9-IN-2 or 500 nM CKDI(7) (3 plates each, total 12 plates). A2058 and U-87-MG: 0 timepoint: Untreated, harvested when compound is added to the other plates (3 plates). 2 hours: DMSO, 500 nM CDK9-IN-2 (3 plates each, total 6 plates). 8 hours: DMSO, 500 nM CDK9-IN-2 (3 plates each, total 6 plates).16 hours: DMSO, 500 nM CDK9-IN-2 (3 plates each, total 6 plates). The IC50s arethe analysed[1].

References:

[1]. Michel Faure, et al. Pharmacodynamic markers associated with cyclin-dependent kinase inhibitors. From PCT Int. Appl. (2012), WO 2012131594A1.

Background

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.

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:
[1]. Michel Faure, et al. Pharmacodynamic markers associated with cyclin-dependent kinase inhibitors. From PCT Int. Appl. (2012), WO 2012131594A1.

Chemical Properties

Cas No. 1263369-28-3 SDF
Chemical Name 4-N-[5-chloro-4-[6-[(3-fluorophenyl)methylamino]pyridin-2-yl]pyridin-2-yl]cyclohexane-1,4-diamine
Canonical SMILES C1CC(CCC1N)NC2=NC=C(C(=C2)C3=NC(=CC=C3)NCC4=CC(=CC=C4)F)Cl
Formula C23H25ClFN5 M.Wt 425.93
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.3478 mL 11.739 mL 23.478 mL
5 mM 0.4696 mL 2.3478 mL 4.6956 mL
10 mM 0.2348 mL 1.1739 mL 2.3478 mL
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