2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR-IN-82

EGFR-IN-82 (Cmpound 8a) 是一种口服有效的 EGFR 抑制剂，对EGFRL858R/T790M/C797S 和 EGFRDel19/T790M/C797S的 IC50 值分别为 0.09 和 0.06 nM，但对于 EGFRWT 没有明显作用。EGFR-IN-82 具有抗增殖活性并抑制肿瘤生长。EGFR-IN-82 可用于非小细胞肺癌研究。

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EGFR-IN-82 Chemical Structure

EGFR-IN-82 Chemical Structure

CAS No. : 2568086-81-5

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EGFR-IN-82 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

查看所有亚型
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

EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFRWT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research [1].

IC50 & Target

0.09 , 0.06 nM (EGFRL858R/T790M/C797S, EGFRDel19/T790M/C797S)
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
13 nM
Compound: 8h
Antiproliferative activity against mouse BaF3 cells harboring del18/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay
Antiproliferative activity against mouse BaF3 cells harboring del18/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay
[PMID: 35810715]
体外研究
(In Vitro)

EGFR-IN-82 (compound 8a) (72 h) 显著抑制 Ba/F3-EGFRDel19/T790M/C797S 细胞的生长，其 IC50 值为 12.7 nM，但对 A431 细胞的生长无显著作用[1]。

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

EGFR-IN-82 相关抗体:
体内研究
(In Vivo)

EGFR-IN-82 (compound 8a) 体内药代动力学性能优于 Brigatinib (HY-12857)[1]。
EGFR-IN-82 (15 - 30 mg/kg, 口服, 14 - 21 天) 中度抑制 PC9-EGFRDel19/T790M/C797S 异种移植小鼠模型肿瘤的生长，高度抑制 Ba/F3-EGFRDel19/T790M/C797S 异种移植小鼠模型肿瘤的生长[1]。

在 Balb/C 小鼠中的药代动力学分析[1]

Route Dose (mg/kg) Cmax (ng/mL) AUC0-t (ng/mL*h) AUC0-∞(ng/mL*h) t1/2 (h) MRT (h)
p.0. 5 1574 15375 15632 3.5 6

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

Animal Model: PC9-EGFRDel19/T790M/C797S xenograft mice model
Ba/F3-EGFR Del19/T790M/C797S xenograft mice model [1]
Dosage: 15 or 30 mg/kg/day, 14-21 days
Administration: Oral gavage (p.o.)
Result: Exhibited moderate inhibition on tumor growth, with a tumor growth inhibition rate (TGI) of 21.60% at 15 mg/kg and 46.79% at 30 mg/kg in PC9-EGFR Del19/T790M/C797S xenograft mice model. Presented a very strong tumor growth inhibition effect with the TGI of 48.43% at low dose(15 mg/kg) and 82.60% at high dose(30 mg/kg) in xenograft mice model of Ba/F3-EGFR Del19/T790M/C797S.
分子量

694.60

Formula

C32H41BrN9O2P
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

EGFR-IN-82 相关分类

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  • 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:

EGFR-IN-822568086-81-5EGFREpidermal growth factor receptorErbB-1HER1Ba/F3-EGFR（Del19/T790M/C797S）cellsA431 cellsPC9-EGFR（Del19/T790M/C797S）xenograft mice modelxenograft mice model of Ba/F3-EGFR（Del19/T790M/C797S）Inhibitorinhibitorinhibit

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