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YX-2-107
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。
YX-2-107图片
CAS NO:2417408-46-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
YX-2-107 是一种选择性降解CDK6PROTAC(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 aPROTAC(IC50= 4.4 nM) that selectively degradesCDK6. YX-2-107 effectively inhibitsRBphosphorylation andFOXM1expression 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)[1].

IC50& Target[1]

CDK6

4.4 nM (IC50)

体外研究
(In Vitro)

YX-2-107 (2000 nM; 48 h) shows inhibition of S phase in Ph+BV173 and SUP-B15 cells[1].
YX-2-107 (0, 1.6, 8, 40, 200, 1000 nM;4 h) selectively degrades CDK6 in BV173 cells[1].
YX-2-107 (2000 nM; 72 h) inhibits RB phosphorylation and FOXM1 expression in Ph+BV173 and SUP-B15 cells[1].

Cell Cycle Analysis[1]

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

Western Blot Analysis[1]

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[1].
YX-2-107 (150 mg/kg; i.p.; single daily for 3 days) is pharmacologically active in suppressing Ph+ALL proliferation in mice[1].

Animal Model:NRG-SGM3 mice (Ph+ALL xenografts model)[1].
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[1].
Dosage:10 mg/kg
Administration:Intraperitoneal injection; single
Result:1.19Pharmacokinetic Parameters of YX-2-107 in C57BL/6j mice[1].
IP (10 mg/kg)
Tmax(h)0.5
Cmax(ng/mL)660
AUC0-t(ng/mL·h)815
AUC0-∞(ng/mL·h)987
分子量

889.95

Formula

C45H51N11O9

CAS 号

2417408-46-7

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.