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Cat. No.: HY-150562

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CDK9-IN-19

CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC₅₀ value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML).

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

CAS No.: 2479306-60-8
Formula: C₂₆H₂₂F₂N₄O₅
Molecular Weight:508.47

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

CDK9-IN-19 Chemical Structure

CAS No.: 2479306-60-8

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

CDK9/cyclinT1

2 nM (IC₅₀)

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.09 μM Compound: 30i	Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
A549	IC₅₀	0.47 μM Compound: 30i	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
BXPC-3	IC₅₀	0.08 μM Compound: 30i	Antiproliferative activity against human BxPC3 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human BxPC3 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
HCT-116	IC₅₀	0.28 μM Compound: 30i	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
HepG2	IC₅₀	0.1 μM Compound: 30i	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
MDA-MB-231	IC₅₀	0.23 μM Compound: 30i	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
MIA PaCa-2	IC₅₀	0.46 μM Compound: 30i	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
MOLM-13	IC₅₀	0.26 μM Compound: 30i	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
MOLM-13	IC₅₀	0.26 μM Compound: 5	Growth inhibition of human MOLM-13 cells Growth inhibition of human MOLM-13 cells	[PMID: 34415148]
MV4-11	IC₅₀	0.09 μM Compound: 30i	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
MV4-11	IC₅₀	0.09 μM Compound: 5	Growth inhibition of human MV4-11 cells incubated after 72 hrs by CTG- luminescence assay Growth inhibition of human MV4-11 cells incubated after 72 hrs by CTG- luminescence assay	[PMID: 34415148]
NCI-H460	IC₅₀	0.64 μM Compound: 30i	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
NCI-N87	IC₅₀	0.6 μM Compound: 30i	Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
PANC-1	IC₅₀	0.3 μM Compound: 30i	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]
SW-620	IC₅₀	0.43 μM Compound: 30i	Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 32447197]

In Vitro

CDK9-IN-19 (compound 30i) has antiproliferative activity against a panel of human tumor cell lines with IC₅₀ ranks of 0.08~0.64 μM (for example: Hep G2, HCT-116, SW620, A549, MV-4-11, et al.)^[1].
CDK9-IN-19 has low hERG inhibitory activity (IC₅₀=10080 nM) and over 5000-fold selectivity for CDK9^[1].
CDK9-IN-19 (0.1-0.8 μM; 24 h) reduces the expression levels of Mcl-1 and c-Myc^[1].

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

Western Blot Analysis^[1]

Cell Line:

MV4-11
Concentration:

0.1, 0.2, 0.4 and 0.8 μM
Incubation Time:

24 h
Result:

Clearly reduced the expression levels of Mcl-1 and c-Myc at 0.1 μM, and completely reduced at 0.2-0.8 μM.

In Vivo

CDK9-IN-19 (10, 20 or 40 mg/kg; IV, for 32 days) significantly suppresses the tumour progression in MV4-11 xenograft model^[1].
Pharmacokinetic Parameters of CDK9-IN-19 in ICR mice^[1].

	PO (30 mg/kg)	IV (2 mg/kg)
T_1/2 (h)	NR	0.23
T_max (h)	0.25	-
C₀ (ng/mL)	-	3060
C_max (ng/mL)	665	-
AUC_0-t (ng/mL·h)	1200	560
AUC_0-∞ (ng/mL·h)	NR	561
CL (L/h/kg)	-	3.56
Vd_SS (L/kg)	-	0.67
F (%)	14.3	-

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

Animal Model:

Female BALB/c nude mice (injected with MV4-11)^[1]
Dosage:

10, 20 or 40 mg/kg
Administration:

IV, for 32 days
Result:

Significantly suppressed the tumour progression and tumour growth inhibition (TGI) values up to 100% from days 14-32 at 40 mg/kg.

Chemical Information

CAS No. 2479306-60-8
Molecular Weight 508.47
Formula C₂₆H₂₂F₂N₄O₅
SMILES

O=C1C(C(C)=O)=C(N2CCOCC2)C3=C(O1)C=C(NC4=NC=C(F)C(C5=CC=C(F)C=C5OC)=N4)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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)
Handling Instructions (2659 KB)

References

[1]. Xu J, et al. Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity. Eur J Med Chem. 2020 Aug 15;200:112424. [Content Brief]

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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.

Keywords

100 mg

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