2. Cell Cycle/DNA Damage
  3. CDK
  4. PKMYT1-IN-13

PKMYT1-IN-13 是一种强效、口服活性且选择性高的 PKMYT1 抑制剂，在 ADP-Glo 检测中对 PKMYT1 的抑制作用 IC50 值小于 10.0 nM，在 NanoBRET 细胞实验中为 19.9 nM。PKMYT1-IN-13 对 WEE1 表现出高度选择性。PKMYT1-IN-13 在 CCNE1 扩增的细胞中表现出选择性抗增殖活性，而对野生型细胞影响甚微。PKMYT1-IN-13 在 HCC1569 小鼠异种移植模型中展现出显著的抗肿瘤活性。PKMYT1-IN-13 可用于 CCNE1 扩增型癌症的研究，例如胃癌、卵巢癌、乳癌癌。

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PKMYT1-IN-13

PKMYT1-IN-13 Chemical Structure

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PKMYT1-IN-13 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PKMYT1-IN-13 is a potent, orally active and selective PKMYT1 inhibitor that inhibits PKMYT1 with IC50 values < 10.0 nM in ADP-Glo assay and 19.9 nM in NanoBRET cellular assay. PKMYT1-IN-13 exhibits high selectivity over WEE1. PKMYT1-IN-13 shows selective antiproliferative activity in CCNE1-amplified cells, while showing minimal wild-type effects. PKMYT1-IN-13 shows antitumor efficacy in HCC1569 mouse xenografts. PKMYT1-IN-13 can be used for the research of CCNE1-amplified cancers, such as gastric, ovarian, and breast cancer[1].

IC50 & Target[1]

CDK1

8.7 nM (IC50)

PKMYT1

19.9 nM (IC50)

体外研究
(In Vitro)

PKMYT1-IN-13 (compound 20) (7 天) 在 CCNE1 扩增的细胞系 (HCC1569、MKN1、OVCAR-3、AsPc-1、SW837、SW1463 和 DLD-1 FBXW7-/-) 中表现出强效的抗增殖活性，其 IC50 值分别为 29.4、32.8、43.5、83.5、45.9、87.8 和 328.5 nM，而在相应的野生型对照细胞中则表现出极小的抑制效应 (对 SK-OV-3 细胞的 IC50 为 13672 nM，对 DLD-1 亲本细胞的 IC50 > 25000 nM)[1]。
PKMYT1-IN-13 (2 小时) 在 HCC1569 细胞中抑制 CDK1 在 Thr14 位点的磷酸化，其 IC50 为 8.7 nM[1]。
PKMYT1-IN-13 具有良好的安全性特征 (低 CYP 抑制、时间依赖性抑制 (TDI)、hERG 活性) 及高激酶选择性，在对包含 217 种激酶的面板筛选中获得了 S (10) = 0.03 的选择性评分[1]。

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

PKMYT1-IN-13 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 2 nM i.v. CL 2.76 mL/min/kg
Mice[1] 2 nM i.v. Vdss 0.75 L/kg
Mice[1] 2 nM i.v. T1/2 8.05 h
Mice[1] 2 nM i.v. AUC0-t 11528 ng·h/mL
Mice[1] 10 nM p.o. Tmax 0.42 h
Mice[1] 10 nM p.o. Cmax 16580 ng/mL
Mice[1] 10 nM p.o. AUC0-t 25763 ng·h/mL
Mice[1] 10 nM p.o. F 43.0 %
Rat[1] 1 nM i.v. CL 7.24 mL/min/kg
Rat[1] 1 nM i.v. Vdss 0.53 L/kg
Rat[1] 1 nM i.v. T1/2 2.06 h
Rat[1] 1 nM i.v. AUC0-t 2278 ng·h/mL
Rat[1] 10 nM p.o. Tmax 0.25 h
Rat[1] 10 nM p.o. Cmax 3924 ng/mL
Rat[1] 10 nM p.o. AUC0-t 6826 ng·h/mL
Rat[1] 10 nM p.o. F 30 %
Dog[1] 1 nM i.v. CL 8.09 mL/min/kg
Dog[1] 1 nM i.v. Vdss 2.00 L/kg
Dog[1] 1 nM i.v. T1/2 4.30 h
Dog[1] 1 nM i.v. AUC0-t 2053 ng·h/mL
Dog[1] 4 nM p.o. Tmax 0.67 h
Dog[1] 4 nM p.o. Cmax 709 ng/mL
Dog[1] 4 nM p.o. AUC0-t 3416 ng·h/mL
Dog[1] 4 nM p.o. F 47.6 %
Rat[1] 100 nM p.o. Tmax 0.25 h
Rat[1] 100 nM p.o. Cmax 3899 ng/mL
Rat[1] 100 nM p.o. AUClast 25765 ng·h/mL
Rat[1] 100 nM p.o. AUCinf 26901 ng·h/mL
Rat[1] 30 nM p.o. Cmax 1104 ng/mL
Rat[1] 30 nM p.o. AUClast 9780 ng·h/mL
Rat[1] 30 nM p.o. AUCinf 9858 ng·h/mL
Rat[1] 30 nM p.o. F 14 %
Rat[1] 200 nM p.o. Cmax 2721 ng/mL
Rat[1] 200 nM p.o. AUClast 24783 ng·h/mL
Rat[1] 200 nM p.o. AUCinf 27136 ng·h/mL
Rat[1] 200 nM p.o. F 5 %
体内研究
(In Vivo)

PKMYT1-IN-13 (compound 20) (10 和 20 mg/kg；口服；每日两次，连续 26 天) 在 HCC1569 异种移植小鼠模型中表现出剂量依赖性的抗肿瘤活性[1]。

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

Animal Model: Female NOD-SCID (6-8 weeks old) subcutaneoously implanted with HCC1569 cells[1]
Dosage: 10; 20 mg/kg
Administration: p.o.; twice daily for 26 days
Result: Induced dose-dependent tumor growth inhibition (TGI) with 66% TGI at 10 mg/kg and 86% TGI at 20 mg/kg.
Showed sustained inhibition of pCDK1(T14) over 24 hours postdose.
Maintained unbound plasma concentrations above the pCDK1(T14) IC90 threshold for most of the dosing interval.
Was tolerated at both dose levels, with a mean body weight loss of 8%.
分子量

424.45

Formula

C24H20N6O2
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.
纯度 & 产品资料
参考文献

PKMYT1-IN-13 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PKMYT1-IN-13CDKCyclin dependent kinaseCDK1 pThr14NOD-SCID miceWEE1HCC1569 xenograftsCCNE1-amplified cellsCCNE1-amplified cancersHCC1569 mouse xenograftgastric cancerbreast cancerovarian cancerInhibitorinhibitorinhibit

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产品名称：
PKMYT1-IN-13
目录号：
HY-181004
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