2479306-60-8

Name	2H-1-Benzopyran-2-one, 3-acetyl-7-[[5-fluoro-4-(4-fluoro-2-methoxyphenyl)-2-pyrimidinyl]amino]-4-(4-morpholinyl)-
CAS	2479306-60-8
Molecular Formula	C26H22F2N4O5
Molecular Weight	508.47
MOL File	2479306-60-8.mol

Synonyms

CDK9-IN-19 2H-1-Benzopyran-2-one, 3-acetyl-7-[[5-fluoro-4-(4-fluoro-2-methoxyphenyl)-2-pyrimidinyl]amino]-4-(4-morpholinyl)-

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Chemical Properties

Boiling point	682.9±65.0 °C(Predicted)
density	1.425±0.06 g/cm3(Predicted)
pka	0.35±0.10(Predicted)

Hazard Information

Uses

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)[1].

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	-

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.

IC 50

CDK9/cyclinT1: 2 nM (IC₅₀)

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. DOI:10.1016/j.ejmech.2020.112424

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