Cat. No.: HY-16462

CDK9-IN-2

Name: CDK9-IN-2
Brand: MedChemExpress
SKU: HY-16462
Price: 240.00 USD
Availability: InStock
Rating: 5 (7 reviews)

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

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.

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Pureté : 98.72%
CAS No.: 1263369-28-3
Formule: C₂₃H₂₅ClFN₅
Masse moléculaire:425.93

Stockage:

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

CDK9-IN-2 Chemical Structure

CAS No.: 1263369-28-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (7)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

sup>[1]

CDK9

5 nM (IC₅₀, H929 multiple myeloma cell line)

Voir tous les produits spécifiques à Isoform CDK :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.116 μM Compound: I-CDK9	Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
A498	IC₅₀	0.057 μM Compound: 30; CDK9	Antiproliferative activity against human A498 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A498 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 38564299]
A549	IC₅₀	1.62 μM Compound: I-CDK9	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
AD293	IC₅₀	0.076 μM Compound: 30; CDK9	Antiproliferative activity against human A-293 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay Antiproliferative activity against human A-293 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay	[PMID: 38564299]
BT-549	IC₅₀	0.053 μM Compound: I-CDK9	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
HeLa	IC₅₀	0.15 μM Compound: I-CDK9	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
HepG2	IC₅₀	0.473 μM Compound: I-CDK9	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
HK-2	IC₅₀	0.187 μM Compound: I-CDK9	Cytotoxicity against HK-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against HK-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
Hs-578T	IC₅₀	0.074 μM Compound: I-CDK9	Antiproliferative activity against human Hs-578T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human Hs-578T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
L02	IC₅₀	0.278 μM Compound: I-CDK9	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
MCF-10A	IC₅₀	0.108 μM Compound: I-CDK9	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
MDA-MB-231	IC₅₀	0.08 μM Compound: I-CDK9	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
MRC5	IC₅₀	0.197 μM Compound: I-CDK9	Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]

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. .

Chemical Information

CAS No. 1263369-28-3
Appearance Solid
Masse moléculaire 425.93
Formule C₂₃H₂₅ClFN₅
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (7)

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Journal Impact Factor

Cancer Discov

Enhancer Remodeling during Adaptive Bypass to MEK Inhibition Is Attenuated by Pharmacologic Targeting of the P-TEFb Complex. [Abstract]

2017 Mar;7(3):302-321. PMID: 28108460

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.
Nat Cancer

Targeting the ALK-CDK9-Tyr19 kinase cascade sensitizes ovarian and breast tumors to PARP inhibition via destabilization of the P-TEFb complex. [Abstract]

2022 Oct;3(10):1211-1227. PMID: 36253486
Cell Host Microbe

Transcriptional Elongation of HSV Immediate Early Genes by the Super Elongation Complex Drives Lytic Infection and Reactivation from Latency. [Abstract]

2017 Apr 12;21(4):507-517.e5. PMID: 28407486
Cancer Res

SMARCA4 loss increases RNA Polymerase II pausing and elevates R-loops to inhibit BRCA1-mediated repair in ovarian cancer. [Abstract]

2025 May 14. PMID: 40366633
SLAS Discov

Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth. [Abstract]

2018 Sep;23(8):850-861. PMID: 29742358
PLoS One

BIRC6 mediates imatinib resistance independently of Mcl-1. [Abstract]

2017 May 16;12(5):e0177871. PMID: 28520795

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.
Res Sq

2026 Jan 6.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Bioz

Keywords

CDK9-IN-2

7 Cited Publications

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CDK9-IN-2

Publications Citing Use of MedChemExpress (MCE) CDK9-IN-2

Voir tous les produits spécifiques à Isoform CDK