TRK-IN-23
TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC50 values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKAG595R, TRKAF589L, and TRKAG667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2924344-29-4
- 分子式: C20H17FN4O2
- 分子量:364.37
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
TrkA 0.5 nM (IC50) |
TrkC 9 nM (IC50) |
TRKAG595R 14 nM (IC50) |
TRKAF589L 4.4 nM (IC50) |
TRKAG667C 4.8 nM (IC50) |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
187.2 nM
Compound: 24b
|
Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37030091] |
| BaF3 | IC50 |
4.5 nM
Compound: 24b
|
Antiproliferative activity against mouse BaF3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37030091] |
| BaF3 | IC50 |
41.5 nM
Compound: 24b
|
Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37030091] |
| KM12 | IC50 |
11.4 nM
Compound: 24b
|
Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37030091] |
化学情報
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CAS 番号 2924344-29-4
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分子量 364.37
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分子式 C20H17FN4O2
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SMILES
COC1=CC=C(C=C1CNC2=CC3=C(NC(/C3=C\C4=CN=CN4)=O)C=C2)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)