CDK9-IN-19

立即咨询

CDK9-IN-19

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2479306-60-8

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

CDK9-IN-19 是高效且具有选择性的CDK9抑制剂，IC₅₀为 2.0 nM。CDK9-IN-19 具有良好的癌细胞抗增殖活性、中等药代动力学特性和较低的 hERG 抑制活性。CDK9-IN-19 在 MV4-11 异种移植小鼠模型中显著抑制肿瘤生长。CDK9-IN-19可用于研究急性髓系白血病 (AML) 。

生物活性

CDK9-IN-19 is a highly potent and selectiveCDK9inhibitor with anIC₅₀value 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].

IC₅₀& Target^[1]

CDK9/cyclinT1

2 nM (IC₅₀)

体外研究
(In Vitro)

CDK9-IN-19 (compound 30i) has antiproliferative activity against a panel of human tumor cell lines with IC₅₀ranks 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].

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.

体内研究
(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.

分子量

508.47

Formula

C₂₆H₂₂F₂N₄O₅

CAS 号

2479306-60-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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