2. Cell Cycle/DNA Damage
  3. Wee1
  4. PKMYT1-IN-9

PKMYT1-IN-9 是一种高选择性、具有口服活性的 PKMYT1 (IC50: 4.4 nM) 抑制剂。PKMYT1-IN-9 对 PKMYT1 的选择性高于 WEE1 (IC50: 32.4 μM)。PKMYT1-IN-9 具有抗肿瘤活性。

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PKMYT1-IN-9 Chemical Structure

PKMYT1-IN-9 Chemical Structure

CAS No. : 3055031-36-9

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PKMYT1-IN-9 相关抗体

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PKMYT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PKMYT1-IN-9 is a highly selective and orally active PKMYT1 inhibitor (IC50: 4.4 nM). PKMYT1-IN-9 shows more selective for PKMYT1 than WEE1 (IC50: 32.4 μM). PKMYT1-IN-9 exhibits antitumor activity[1].

IC50 & Target[1]

PKMYT1

4.4 nM (IC50)

体外研究
(In Vitro)

PKMYT1-IN-9 (Compound 36) (7 天) 对 HCC1569 细胞系 (CC50: 0.31 μM) 有较强的抗增殖效应，对 KYSE30 细胞系 (CC50: >30 μM) 的抗增殖效应较弱[1]。
PKMYT1-IN-9 对 EPHA1 激酶有强抑制作用 (IC50: 10.1 nM)，但对其他六种激酶 (ABL1、ABL2、BRAF、CSF1R、LCK 和 SRC) 的效力较低 (IC50: >60 nM)[1]。
PKMYT1-IN-9 无 GSH 反应性，无 hERG 抑制，对 CYP 抑制率低 (<50%)，在人、小鼠肝微粒体中的清除率高 (77.3 mL/min/kg at 1 mg/kg IV)[1]。

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

PKMYT1-IN-9 相关抗体:
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. CL 43.7 mL/min/kg
Mice 10 mg/kg p.o. AUC0-∞ 1602 ng·h/mL
Mice 1 mg/kg i.v. AUC0-∞ 349.3 ng·h/mL
Mice 10 mg/kg p.o. T1/2 0.77 hr
Mice 1 mg/kg i.v. Vss 0.90 L/kg
Mice 10 mg/kg p.o. Cmax 1923.7 ng/mL
Mice 1 mg/kg i.v. T1/2 0.26 hr
Mice 10 mg/kg p.o. Tmax 0.3 hr
Mice 1 mg/kg i.v. Cmax 898.0 ng/mL
Mice 10 mg/kg p.o. F 45.8 %
Mice 1 mg/kg i.v. Tmax 0.1 hr
体内研究
(In Vivo)

PKMYT1-IN-9 (Compound 36) (15 mg/kg，口服，每日 2 次，21 天) 可抑制 HCC1569 衍生肿瘤异种移植 (CDX) 小鼠模型中雌性 NOD-SCID 小鼠肿瘤的生长 (53%)[1]。

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

Animal Model: CCNE1-amplified cell line HCC1569-derived tumor xenograft (CDX) mouse model, female NOD-SCID mice (6–8 weeks old; Vital River)[1]
Dosage: 15 mg/kg
Administration: Oral gavage (p.o.), twice daily for 21 d
Result: Inhibited tumor growth (53%).
Slightly reduced the total body weight of mouse (10%).
Shows similar pCDK1 IC50 coverage as RP-6306 over 8 h in vitro.
The quantified tumor CDK1-pT14 level was 52%.
分子量

323.32

Formula

C17H14FN5O
CAS 号
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-9 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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-93055031-36-9Wee1AntitumorHCC1569KYSE30HCC1569 xenograftCDX mouse modelInhibitorinhibitorinhibit

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目录号：
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