YX-2-107

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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).

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.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.

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.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.

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Others

Other Targets

PROTACs | CDK

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2417408-46-7

889.95

C45H51N11O9

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (112.37 mM; 超声助溶 )

O=C1NC(=O)C(N2C(=O)C=3C=CC=C(OCC(=O)NCCCCNCC(=O)N4CCN(C5=CN=C(C=C5)NC=6N=CC7=C(N6)N(C(=O)C(C(=O)C)=C7C)C8CCCC8)CC4)C3C2=O)CC1

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(-20℃)

With Ice Pack

≥ 2 years