2. Protein Tyrosine Kinase/RTK
  3. c-Kit
  4. c-Kit-IN-2

c-Kit-IN-2 是一种 c-KIT 抑制剂，IC50 值为 82 nM，对三种 GIST 细胞系 GIST882、GIST430 和 GIST48 均有较好的抗增殖活性，GI50 值分别为 3、1 和 2 nM。

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c-Kit-IN-2 Chemical Structure

c-Kit-IN-2 Chemical Structure

CAS No. : 2121515-37-3

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c-Kit-IN-2 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

c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively[1].

IC50 & Target

IC50: 82 nM (c-KIT)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 GI50
14.6 μM
Compound: 10a
Antiproliferative activity against human A549 assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human A549 assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 30968693]
Detroit 551 GI50
> 10 μM
Compound: 10a
Antiproliferative activity against human Detroit 551 assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human Detroit 551 assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 30968693]
GIST430 GI50
1 nM
Compound: 10a
Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by MTS assay
Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by MTS assay
[PMID: 30968693]
GIST430 GI50
1 nM
Compound: 10a
Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by methylene blue staining based ass
Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by methylene blue staining based ass
[PMID: 30968693]
GIST48 GI50
2 nM
Compound: 10a
Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by MTS assay
Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by MTS assay
[PMID: 30968693]
GIST48 GI50
2 nM
Compound: 10a
Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by methylene blue staining based assay
Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by methylene blue staining based assay
[PMID: 30968693]
GIST882 GI50
3 nM
Compound: 10a
Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by MTS assay
Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by MTS assay
[PMID: 30968693]
GIST882 GI50
3 nM
Compound: 10a
Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by methylene blue staining based assay
Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by methylene blue staining based assay
[PMID: 30968693]
GISTT1 GI50
2.2 nM
Compound: 10a
Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 deletion mutant assessed as reduction in cell viability by MTS assay
Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 deletion mutant assessed as reduction in cell viability by MTS assay
[PMID: 30968693]
GISTT1 GI50
2.2 nM
Compound: 10a
Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 del mutation assessed as reduction in cell viability by methylene blue staining based assay
Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 del mutation assessed as reduction in cell viability by methylene blue staining based assay
[PMID: 30968693]
PC-3 GI50
> 20 μM
Compound: 10a
Antiproliferative activity against human PC3 assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human PC3 assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 30968693]
Sf9 IC50
69 nM
Compound: 10a
Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30
Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30
[PMID: 30968693]
Sf9 IC50
82 nM
Compound: 10a
Inhibition of recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation measured after 150 mins in pr
Inhibition of recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation measured after 150 mins in pr
[PMID: 30968693]
Sf9 IC50
92 nM
Compound: 10a
Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 3
Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 3
[PMID: 30968693]
分子量

519.62

Formula

C25H29N9O2S
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

c-Kit-IN-2 相关分类

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  • 稀释计算器

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× = ×
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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:

c-Kit-IN-22121515-37-3c-KitSCFRCD117Inhibitorinhibitorinhibit

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