1. Cell Cycle/DNA Damage Apoptosis
  2. Wee1 Apoptosis
  3. PKMYT1-IN-10

PKMYT1-IN-10 是一种选择性的 PKMYT1 抑制剂,其 IC50 为 3 nM。PKMYT1-IN-10 可抑制克隆形成,诱导细胞凋亡 (apoptosis),并诱导癌细胞周期停滞于 S 期。PKMYT1-IN-10 具有良好的肝微粒体稳定性和血浆稳定性,且对 CYPs 的抑制作用极小。PKMYT1-IN-10 可用于卵巢癌和乳腺癌的研究。

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PKMYT1-IN-10

PKMYT1-IN-10 Chemical Structure

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查看 Wee1 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PKMYT1-IN-10 is a selective PKMYT1 inhibitor with an IC50 of 3 nM. PKMYT1-IN-10 inhibits colony formation, induces apoptosis, and induces S-phase cancer cell cycle arrest. PKMYT1-IN-10 exhibits liver microsomal stability, favorable plasma stability, minimal CYPs inhibition. PKMYT1-IN-10 can be used for the studies of ovarian cancer and breast cancer[1].

IC50 & Target[1]

PKMYT1

3 nM (IC50)

体外研究
(In Vitro)

PKMYT1-IN-10 (Compound A30) 表现出强效的细胞抑制活性,在 OVCAR3、HCC1569 和 A549 细胞系中的 IC50 值分别为 0.32 μM、0.33 μM 和 > 8 μM[1]
PKMYT1-IN-10 (0.125-2 μM, 14 days) 可抑制 OVCAR3 和 HCC1569 细胞中的集落形成,EC50 分别为 0.37 和 0.35 μM[1]
PKMYT1-IN-10 (0.3-2.4 μM, 5 days) 可诱导 HCC1569 细胞凋亡,并在 HCC1569 细胞和 OVCAR3 中诱导 S 期特异性细胞周期停滞[1]
PKMYT1-IN-10 (37.5-600 nM) 与 Gemcitabine (HY-17026) 表现出高度协同作用,在 HCC1569 细胞和 OVCAR3 细胞中的联合指数 (CI) 值分别为 < 0.5 和 0.5-0.8[1]

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

Apoptosis Analysis[1]

Cell Line: HCC1569 cells
Concentration: 0.3, 0.6 and 1.2 μM
Incubation Time: 5 days
Result: Reached the apoptosis rate by 54.7% at a concentration of 2.4 μM in HCC1569 cells.

Cell Cycle Analysis[1]

Cell Line: HCC1569 cells and OVCAR3 cells
Concentration: 0.3, 0.6 and 1.2 μM
Incubation Time: 5 days
Result: Increased the proportion of cells in the S phase, without causing the typical G2/M arrest.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 3 mg/kg i.v. T1/2 0.20 h
Mice 30 mg/kg p.o. T1/2 0.70 h
Mice 3 mg/kg i.v. Tmax 0.08 h
Mice 30 mg/kg p.o. Tmax 0.33 h
Mice 3 mg/kg i.v. Cmax 622 ng/mL
Mice 30 mg/kg p.o. Cmax 721 ng/mL
Mice 3 mg/kg i.v. AUC0-t 188 ng·h/mL
Mice 30 mg/kg p.o. AUC0-t 497 ng·h/mL
Mice 3 mg/kg i.v. AUC0-∞ 191 ng·h/mL
Mice 30 mg/kg p.o. AUC0-∞ 504 ng·h/mL
Mice 3 mg/kg i.v. MRT0-t 0.12 h
Mice 30 mg/kg p.o. MRT0-t 0.57 h
Mice 3 mg/kg i.v. MRT0-∞ 0.14 h
Mice 30 mg/kg p.o. MRT0-∞ 0.63 h
Mice 3 mg/kg i.v. Vz 4584 mL/kg
Mice 30 mg/kg p.o. F 26.44 %
Mice 3 mg/kg i.v. CL 263 mL/min/kg
分子量

453.51

Formula

C22H23N5O4S

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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)
× = ×
C1   V1   C2   V2
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.

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产品名称:
PKMYT1-IN-10
目录号:
HY-175817
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