2. Protein Tyrosine Kinase/RTK
  3. Itk
  4. ITK inhibitor 6

ITK inhibitor 6 (compound 43) 是一种有效的选择性 ITK 抑制剂，ITK、BTK、JAK3、EGFR、LCK 的 IC50s 分别为 4 nM、133 nM、320 nM、2360 nM、155 nM。ITK inhibitor 6 抑制 PLCγ1 和 ERK1/2 的磷酸化。ITK inhibitor 6 具有抗增殖活性。

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ITK inhibitor 6 Chemical Structure

ITK inhibitor 6 Chemical Structure

CAS No. : 2404604-06-2

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ITK inhibitor 6 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities[1].

IC50 & Target

IC50: 4 nM (ITK); 133 nM (BTK), 320 nM (JAK3), 2360 nM (EGFR), 155 nM (LCK)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CCRF-CEM GI50
3.4 μM
Compound: 43
Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay
Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay
[PMID: 31830635]
H9 GI50
5.4 μM
Compound: 43
Antiproliferative activity against human H9 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay
Antiproliferative activity against human H9 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay
[PMID: 31830635]
HEK-293T GI50
19 μM
Compound: 43
Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay
Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay
[PMID: 31830635]
Jurkat EC50
119 nM
Compound: 43
Inhibition of ITK in anti-CD3/CD28 beads-stimulated human Jurkat cells assessed as reduction in Plcgamma1 phosphorylation incubated for 2 hrs followed by stimulation with anti-CD3/CD28 beads by Western blot analysis
Inhibition of ITK in anti-CD3/CD28 beads-stimulated human Jurkat cells assessed as reduction in Plcgamma1 phosphorylation incubated for 2 hrs followed by stimulation with anti-CD3/CD28 beads by Western blot analysis
[PMID: 31830635]
Jurkat GI50
5.1 μM
Compound: 43
Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay
Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay
[PMID: 31830635]
MOLT-4 GI50
3.7 μM
Compound: 43
Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay
Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay
[PMID: 31830635]
体外研究
(In Vitro)

ITK inhibitor 6 (compound 43) shows antiproliferative activities with GI50s of 5.1, 3.7, 3.4, 5.4, 19 µM for Jurkat, Molt-4, CCRF-CEM, H9, HEK 293 T cells, respectively[1].
ITK inhibitor 6 docks into the ATP-binding site of ITK and BTK[1].

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

ITK inhibitor 6 相关抗体:
分子量

486.51

Formula

C28H24F2N4O2
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

ITK inhibitor 6 相关分类

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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:

ITK inhibitor 62404604-06-2ITK inhibitor6ITK inhibitor-6ItkInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseICR miceHEK 293 TJurkat cellsPLCγ1ERK1/2phosphorylation， antiproliferativeInhibitorinhibitorinhibit

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