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 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] | |
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. |
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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 |
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| 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. |
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