2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK MAPK/ERK Pathway
  3. EGFR c-Met/HGFR p38 MAPK
  4. (R)-Afatinib

(R)-Afatinib  (Synonyms: (R)-BIBW 2992)

目录号: HY-10261E
产品使用指南 技术支持

(R)-Afatinib ((R)-BIBW 2992) 是 Afatinib 异构体。Afatinib (HY-10261) 是一种口服有效且不可逆的 ErbB 家族 (EGFR和HER2) 双特异性抑制剂，对 EGFRwt, EGFRL858R, EGFRL858R/T790M 和 HER2 的 IC50 值分别为 0.5 nM、0.4 nM、10 nM 和 14 nM。Afatinib 可用于食管鳞状细胞癌 (ESCC)、非小细胞肺癌 (NSCLC) 和胃癌的研究。

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(R)-Afatinib Chemical Structure

(R)-Afatinib Chemical Structure

CAS No. : 439081-17-1

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Other Forms of (R)-Afatinib:

(R)-Afatinib 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

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

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 IC50
< 0.001 μM
Compound: BIBW2992
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
[PMID: 28987609]
A549 IC50
0.71 μM
Compound: 3
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
[PMID: 29775935]
BT-474 IC50
54 nM
Compound: 34; BIBW2992
Antiproliferative activity against human BT474 cells expressing wild type HER2 incubated for 72 hrs by MTS assay
Antiproliferative activity against human BT474 cells expressing wild type HER2 incubated for 72 hrs by MTS assay
[PMID: 28754471]
MCF7 IC50
0.93 μM
Compound: 3
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
[PMID: 29775935]
NCI-H1975 IC50
0.495 μM
Compound: BIBW2992
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
[PMID: 28987609]
NCI-H1975 IC50
92 nM
Compound: 34; BIBW2992
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay
[PMID: 28754471]
PC-3 IC50
2.51 μM
Compound: 3
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
[PMID: 29775935]
分子量

485.94

Formula

C24H25ClFN5O3
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

(R)-Afatinib 相关分类

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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.

Keywords:

(R)-Afatinib439081-17-1(R)-BIBW 2992EGFRc-Met/HGFRp38 MAPKEpidermal growth factor receptorErbB-1HER1isomerHER2anticancerorally activelung cancerInhibitorinhibitorinhibit

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