CDK9-IN-19

Cat. No.: HY-150562: FAQs
Data Sheet Handling Instructions

Molarity Calculator

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.

CDK9-IN-19 Chemical Structure

CAS No. : 2479306-60-8

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CDK9/cyclinT1

2 nM (IC₅₀)

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]
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.

Molecular Weight

508.47

Formula

C₂₆H₂₂F₂N₄O₅

CAS No.

2479306-60-8

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

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]

CDK9-IN-19 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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-192479306-60-8CDKCyclin dependent kinaseanticancerantiproliferativeantitumorMV4-11AMLCDK9BALB/c micexenograftInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks