2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. SH-1092

SH-1092 是一种具有口服活性的 EGFR 抑制剂，对 EGFRT790M/L858R 的 IC50 为 0.96 nM，对野生型 EGFR 的 IC50 为 6.1 nM。SH-1092 对非小细胞肺癌具有抗癌活性。SH-1092 可用于非小细胞肺癌的相关研究。

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SH-1092

SH-1092 Chemical Structure

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SH-1092 相关抗体

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SH-1092 is an orally active EGFR inhibitor with an IC50 of 0.96 nM against EGFRT790M/L858R and an IC50 of 6.1 nM against wild-type EGFR. SH-1092 exhibits anticancer activity against non-small cell lung cancer. SH-1092 can be used in studies related to non-small cell lung cancer[1].

IC50 & Target[1]

EGFRL858R/T790M

0.96 nM (IC50)

EGFR (WT)

EGFR nM (IC50)

体外研究
(In Vitro)

SH-1092 可强效抑制 EGFRT790M/L858R，其 IC50 为 0.96 nM；它还可抑制野生型 EGFR，IC50 为 6.1 nM，对突变型具有中等选择性，且对 IGF1R 和 INSR 仅表现出微弱的抑制作用[1]。
SH-1092 (0.1 nM-10 μM; 72 h) 可抑制 H1975 (EGFRT790M/L858R) 细胞和 A431 (野生型 EGFR) 细胞的增殖[1]。

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

SH-1092 相关抗体:

Cell Proliferation Assay[1]

Cell Line: H1975 (EGFR T790M/L858R mutant) non-small cell lung cancer cell line, A431 (EGFR wild-type) non-small cell lung cancer cell line
Concentration: 0.1 nM-10 μM
Incubation Time: 72 h
Result: Inhibited the growth of H1975 cells with an IC50 of 8 nM.
Inhibited the growth of A431 cells with an IC50 of 362 nM.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUC0-t AUC0-∞ CL Tmax F
Mice[1] 1.25 mg/mL p.o. 2.7 h 1062 ng·h/mL 1092.9 ng·h/mL / 0.8 h 19.8 %
Mice[1] 0.2 mg/mL i.v. 0.5 h 429.1 ng·h/mL 429.4 ng·h/mL 4.9 L/h/kg / /
体内研究
(In Vivo)

SH-1092 (25-50 mg/kg；口服；每日一次；连续 14 天) 对雌性 BALB/c 裸鼠体内 EGFR 野生型 A431 非小细胞肺癌异种移植物表现出剂量依赖性的显著抗肿瘤活性，且急性毒性较低[1]。
SH-1092 (10-50 mg/kg；口服；每日一次；连续 14 天) 在雌性 BALB/c 裸鼠中对 EGFRT790M/L858R 突变型 H1975 非小细胞肺癌异种移植物表现出剂量依赖性的显著抗肿瘤活性，且急性毒性较低[1]。

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

Animal Model: BALB/c nude (female)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: p.o.; daily; 14 days
Result: Significantly inhibited A431 xenograft tumor growth in a dose-dependent manner.
Did not change mouse body weight significantly during treatment, indicating low acute toxicity.
Animal Model: BALB/c nude (female)[1]
Dosage: 10 mg/kg; 25 mg/kg; 50 mg/kg
Administration: p.o.; daily; 14 days
Result: Significantly inhibited H1975 xenograft tumor growth in a dose-dependent manner.
Did not change mouse body weight significantly during treatment, indicating low acute toxicity.
分子量

541.64

Formula

C30H35N7O3
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

SH-1092 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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

SH-1092SH1092SH 1092EGFREpidermal growth factor receptorErbB-1HER1CYP1A2INSRIGF1Rnon-small cell lung cancerA431 cellsEGFR (T790M/L858R)CYP3A4CYP2D6EGFR (wild-type)H1975 cellsInhibitorinhibitorinhibit

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目录号：
HY-183292
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