CDK4/6-IN-15|cas:2078047-99-9|西域试剂

CDK4/6-IN-15

产品编号：Bellancom-142076| CAS NO：2078047-99-9| 分子式：C₂₁H₂₇FN₈S| 分子量：442.56

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货号	价格	库存与货期
Bellancom-142076	￥3000.00	杭州北京（现货）
Bellancom-142076	￥4800.00	杭州北京（现货）
Bellancom-142076	￥9500.00	杭州北京（现货）
Bellancom-142076	￥15000.00	杭州北京（现货）

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CDK4/6-IN-15

产品介绍

CDK4/6-IN-15 是一种口服有效和选择性 CDK4/6 抑制剂。CDK4/6-IN-15 能有效抑制癌细胞生长。CDK4/6-IN-15 将细胞周期阻滞在 G1 期，并抑制视网膜母细胞瘤肿瘤抑制蛋白 (Rb) 在 S780 位点的磷酸化和 E2 因子 (E2F) 调控的基因表达。

生物活性

CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression.

体外研究

CDK4/6-IN-15 (compound 91) (10 μM; 24 h) also potently inhibits FLT3 and MYLK4 with inhibition rates >90%.
CDK4/6-IN-15 (0-5 μM; 72 h) suppresses tumour cell proliferation selectively with GI₅₀s of 0.107 μM (MV4-11) and 0.325 μM (MDA-MB-453).
CDK4/6-IN-15 (0.1-1 μM; 24 h) arrests exclusively the cell cycle at G1 phase in Rb-positive MV4-11 cells and MDA-MB-453 cells.
CDK4/6-IN-15 (0.1-1 μM or 0.3-3 μM; 24-96 h) triggers apoptosis in MV4-11 and MDA-MB-453 cells.
CDK4/6-IN-15 (0.1-3.3 μM; 4-24 h) inhibits phosphorylation of Rb.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line:	MV4-11 and MDA-MB-453 cells
Concentration:	0.1 μM, 0.5 μM, and 1 μM for MV4-11; 0.3 μM, 0.6 μM, and 3.3 μM for MDA-MB-453 cells
Incubation Time:	24 h, 48 h, 72 h, and 96 h
Result:	Induced cell apoptosis via arresting cell cycle at G1 accompanied with Rb) phosphorylation suppression and E2F-regulated gene expression decreases.

Western Blot Analysis

Cell Line:	MV4-11 (GI₅₀=0.107 μM) and MDA-MB-453 (GI₅₀=0.325 μM)
Concentration:	1×, 5×, 10× GI₅₀
Incubation Time:	4 h, 12 h, and 24 h
Result:	Resulted inhibition of Rb phosphorylation at S780.

体内研究
(In Vivo)

CDK4/6-IN-15 (compound 91) (2 mg/kg for i.v. or 10 mg/kg for p.o.; single dose) shows comparable oral absorption in healthy male adult BALB/c mice (20-25 g) as well as (5 mg/kg for i.v. or 200 mg/kg for p.o.; single dose) in male albino Wistar rats (250-350 g).

Pharmacokinetic Analysis

	Route	Dose (mg/kg)	CL (mL/min/kg)	V_ss (L/kg)	AUC (μM·h)	C_max (μM)	T_max (h)	t_1/2 (h)	F (%)
rat	IV	5	155	27.5	1.2	1.4	/	2.1	/
	PO	20	/	/	4.4	0.3	4.3	20.3	95
mouse	IV	2	90	15.7	0.7	1.3	/	2.9	/
	PO	10	/	/	4.3	0.6	2.5	2.7	129

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

	Route	Dose (mg/kg)	CL (mL/min/kg)	V_ss (L/kg)	AUC (μM·h)	C_max (μM)	T_max (h)	t_1/2 (h)	F (%)
rat	IV	5	155	27.5	1.2	1.4	/	2.1	/
	PO	20	/	/	4.4	0.3	4.3	20.3	95
mouse	IV	2	90	15.7	0.7	1.3	/	2.9	/
	PO	10	/	/	4.3	0.6	2.5	2.7	129

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

	Route	Dose (mg/kg)	CL (mL/min/kg)	V_ss (L/kg)	AUC (μM·h)	C_max (μM)	T_max (h)	t_1/2 (h)	F (%)
rat	IV	5	155	27.5	1.2	1.4	/	2.1	/
	PO	20	/	/	4.4	0.3	4.3	20.3	95
mouse	IV	2	90	15.7	0.7	1.3	/	2.9	/
	PO	10	/	/	4.3	0.6	2.5	2.7	129