YX-2-107|cas:2417408-46-7|西域试剂

YX-2-107,99.13%

产品编号：Bellancom-148530| CAS NO：2417408-46-7| 分子式：C₄₅H₅₁N₁₁O₉| 分子量：889.95

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-148530		￥5000.00	杭州北京（现货）
Bellancom-148530		￥8000.00	杭州北京（现货）

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YX-2-107

产品介绍

YX-2-107 是一种选择性降解 CDK6 的 PROTAC (IC₅₀= 4.4 nM)。YX-2-107 在体外能有效抑制 RB 磷酸化和 FOXM1 表达，并抑制大鼠体内 Ph⁺ ALL 的发展。YX-2-107 可用于 Ph 染色体阳性 (Ph⁺) 急性淋巴细胞白血病 (ALL) 的研究。

生物活性

YX-2-107 is a PROTAC (IC₅₀= 4.4 nM) that selectively degrades CDK6. YX-2-107 effectively inhibits RB phosphorylation and FOXM1 expression in vitro and inhibits the development of Ph⁺ ALL in rats. YX-2-107 can be used in the study of Ph chromosome-positive (Ph⁺) acute lymphoblastic leukemia (ALL).

体外研究

YX-2-107 (2000 nM; 48 h) shows inhibition of S phase in Ph⁺ BV173 and SUP-B15 cells.
YX-2-107 (0, 1.6, 8, 40, 200, 1000 nM;4 h) selectively degrades CDK6 in BV173 cells.
YX-2-107 (2000 nM; 72 h) inhibits RB phosphorylation and FOXM1 expression in Ph⁺ BV173 and SUP-B15 cells.

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

Cell Cycle Analysis

Cell Line:	Ph⁺ BV173 and SUP-B15 cells
Concentration:	2000 nM
Incubation Time:	48 h
Result:	Inhibited S-phase entry.

Western Blot Analysis

Cell Line:	Ph⁺ BV173 and SUP-B15 cells
Concentration:	2000 nM
Incubation Time:	72 h
Result:	Inhibited the phosphorylation of RB and the expression of FOXM1.

体内研究
(In Vivo)

YX-2-107 (10 mg/kg; i.p.; single) shows a maximum concentration of 741 nM (150-fold greater than CDK6 degradation IC₅₀), with clearance from the plasma after 4 hours.
YX-2-107 (150 mg/kg; i.p.; single daily for 3 days) is pharmacologically active in suppressing Ph⁺ ALL proliferation in mice.

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

Animal Model:	NRG-SGM3 mice (Ph⁺ ALL xenografts model).
Dosage:	150 mg/kg
Administration:	Intraperitoneal injection; single daily for 3 days
Result:	Suppressed the percentage of primary Ph⁺ ALL S-phase cells, the expression of CDK4/6-regulated phospho-RB and, to a lesser degree, FOXM1, and induced the selective CDK6 degradation.

Animal Model:

C57BL/6j mice.

Dosage:

10 mg/kg

Administration:

Intraperitoneal injection; single

Result:

1.19 Pharmacokinetic Parameters of YX-2-107 in C57BL/6j mice .

	IP (10 mg/kg)
T_max (h)	0.5
C_max (ng/mL)	660
AUC_0-t (ng/mL·h)	815
AUC_0-∞ (ng/mL·h)	987

体内研究

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

Animal Model:	NRG-SGM3 mice (Ph⁺ ALL xenografts model).
Dosage:	150 mg/kg
Administration:	Intraperitoneal injection; single daily for 3 days
Result:	Suppressed the percentage of primary Ph⁺ ALL S-phase cells, the expression of CDK4/6-regulated phospho-RB and, to a lesser degree, FOXM1, and induced the selective CDK6 degradation.

Animal Model:

C57BL/6j mice.

Dosage:

10 mg/kg

Administration:

Intraperitoneal injection; single

Result:

1.19 Pharmacokinetic Parameters of YX-2-107 in C57BL/6j mice .

	IP (10 mg/kg)
T_max (h)	0.5
C_max (ng/mL)	660
AUC_0-t (ng/mL·h)	815
AUC_0-∞ (ng/mL·h)	987

体内研究

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

Animal Model:	NRG-SGM3 mice (Ph⁺ ALL xenografts model).
Dosage:	150 mg/kg
Administration:	Intraperitoneal injection; single daily for 3 days
Result:	Suppressed the percentage of primary Ph⁺ ALL S-phase cells, the expression of CDK4/6-regulated phospho-RB and, to a lesser degree, FOXM1, and induced the selective CDK6 degradation.

Animal Model:

C57BL/6j mice.

Dosage:

10 mg/kg

Administration:

Intraperitoneal injection; single

Result:

1.19 Pharmacokinetic Parameters of YX-2-107 in C57BL/6j mice .

	IP (10 mg/kg)
T_max (h)	0.5
C_max (ng/mL)	660
AUC_0-t (ng/mL·h)	815
AUC_0-∞ (ng/mL·h)	987

性状

Solid

溶解性数据

In Vitro:

DMSO : 150 mg/mL (168.55 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.1237 mL	5.6183 mL	11.2366 mL
5 mM	0.2247 mL	1.1237 mL	2.2473 mL
10 mM	0.1124 mL	0.5618 mL	1.1237 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式