CDK9-IN-2

Name: CDK9-IN-2
Brand: MedChemExpress
SKU: HY-16462
Rating: 5.0 (7 reviews)

Cat. No.: HY-16462 Purity: 99.37%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

CDK9-IN-2 Chemical Structure

CAS No. : 1263369-28-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 264	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 264	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 960	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 7 publication(s) in Google Scholar

5 Publications Citing Use of MCE CDK9-IN-2

: CDK9-IN-2 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2017 Mar;7(3):302-321. [Abstract]; Small molecule inhibitor of CDK9, HY-16462, similarly blocks adaptive PDGFRB and DDR1 upregulation. Attenuation of 24 h 100 nM Trametinib-induced PDGFRB and DDR1 upregulation by co-treatment with 100 nM HY-16462.

: CDK9-IN-2 purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 May 16;12(5):e0177871. [Abstract]; Mcl-1 mRNA is similarly reduced. Immunoblot analysis revealed that the highest concentrations of CDK9 inhibitors strongly reduce Mcl-1 protein.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Targetsup>[1]

CDK9

5 nM (IC₅₀, H929 multiple myeloma cell line)

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].

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

Molecular Weight

425.93

Formula

C₂₃H₂₅ClFN₅

CAS No.

1263369-28-3

Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CN=C(N[C@@H]2CC[C@@H](N)CC2)C=C1C3=NC(NCC4=CC(F)=CC=C4)=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (117.39 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	2.3478 mL	11.7390 mL	23.4780 mL
5 mM	0.4696 mL	2.3478 mL	4.6956 mL
10 mM	0.2348 mL	1.1739 mL	2.3478 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (5.87 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 (5.87 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.37%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (254 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

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

Cell Assay
^[1]

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].

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

References

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3478 mL	11.7390 mL	23.4780 mL	58.6951 mL
	5 mM	0.4696 mL	2.3478 mL	4.6956 mL	11.7390 mL
	10 mM	0.2348 mL	1.1739 mL	2.3478 mL	5.8695 mL
	15 mM	0.1565 mL	0.7826 mL	1.5652 mL	3.9130 mL
	20 mM	0.1174 mL	0.5870 mL	1.1739 mL	2.9348 mL
	25 mM	0.0939 mL	0.4696 mL	0.9391 mL	2.3478 mL
	30 mM	0.0783 mL	0.3913 mL	0.7826 mL	1.9565 mL
	40 mM	0.0587 mL	0.2935 mL	0.5870 mL	1.4674 mL
	50 mM	0.0470 mL	0.2348 mL	0.4696 mL	1.1739 mL
	60 mM	0.0391 mL	0.1957 mL	0.3913 mL	0.9783 mL
	80 mM	0.0293 mL	0.1467 mL	0.2935 mL	0.7337 mL
	100 mM	0.0235 mL	0.1174 mL	0.2348 mL	0.5870 mL

CDK9-IN-2 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:

CDK9-IN-21263369-28-3CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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CDK9-IN-2

Customer Review

CDK9-IN-2 Related Antibodies

5 Publications Citing Use of MCE CDK9-IN-2

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

CDK9-IN-2 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CDK9-IN-2 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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