| Company Name: |
Chunchuang (Wuhan) Technology Co., Ltd
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| Tel: |
15727060112 |
| Email: |
yutianchun2007@126.com |
| Products Intro: |
Product Name:2,4-Pyrimidinediamine, 5-chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-[1,2,3,6-tetrahydro-1-(tetrahydro-2H-pyran-4-yl)-4-pyridinyl]phenyl]-
CAS:2196186-84-0
Purity:99.5+
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| Company Name: |
TargetMol Chemicals Inc.
|
| Tel: |
4008200310 |
| Email: |
marketing@tsbiochem.com |
| Products Intro: |
Product Name:APG-2449
CAS:2196186-84-0
Package:25mg/RMB 10600;50mg/RMB 13800;100mg/RMB 17500
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APG-2449 manufacturers
- APG-2449
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- $1520.00 / 25mg
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2024-11-19
- CAS:2196186-84-0
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | APG-2449 Basic information |
| Product Name: | APG-2449 | | Synonyms: | 2,4-Pyrimidinediamine, 5-chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-[1,2,3,6-tetrahydro-1-(tetrahydro-2H-pyran-4-yl)-4-pyridinyl]phenyl]-;APG-2449 | | CAS: | 2196186-84-0 | | MF: | C33H42ClN5O4S | | MW: | 640.24 | | EINECS: | | | Product Categories: | | | Mol File: | 2196186-84-0.mol |  |
| | APG-2449 Chemical Properties |
| Boiling point | 787.4±70.0 °C(Predicted) | | density | 1.271±0.06 g/cm3(Predicted) | | pka | 7.96±0.40(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | APG-2449 Usage And Synthesis |
| Description | APG-2449 is an orally available kinase inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK), focal adhesion kinase (FAK) and the receptor tyrosine kinase C-ros oncogene 1 (ROS1), with potential antineoplastic activity. Upon administration, ALK/FAK/ROS1 inhibitor APG-2449 selectively binds to and inhibits ALK, FAK and ROS1 kinases. The inhibition leads to disruption of ALK-, FAK- and ROS1-mediated signal transduction pathways and eventually inhibits tumor cell growth in ALK-, FAK- and ROS1-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; its dysregulation and gene rearrangements are associated with a variety of tumors. The cytoplasmic tyrosine kinase FAK, a signal transducer for integrins, is upregulated and constitutively activated in various tumor types; it plays a key role in tumor cell migration, proliferation, survival, and tumor angiogenesis. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells. | | Uses | APG-2449 is an orally active inhibitor of ALK/ROS1/FAK. APG-2449 exerts potent and durable antitumor activity in human non-small-cell lung cancer (NSCLC) and ovarian tumor models. | | References | [1] DOUGLAS D FANG. Discovery of a novel ALK/ROS1/FAK inhibitor, APG-2449, in preclinical non-small cell lung cancer and ovarian cancer models.[J]. ACS Applied Electronic Materials, 2022: 752. DOI:10.1186/s12885-022-09799-4.
[2] YUXIANG MA. FAK inhibition with novel FAK/ALK inhibitor APG-2449 could overcome resistance in NSCLC patients who are resistant to second-generation ALK inhibitors.[J]. Journal of Clinical Oncology, 2023. DOI:10.1200/jco.2023.41.16_suppl.9015.
[3] HONGYUN ZHAO. First-in-human phase I results of APG-2449, a novel FAK and third-generation ALK/ ROS1 tyrosine kinase inhibitor (TKI), in patients (pts) with second-generation TKI-resistant ALK/ROS1+ non–small cell lung cancer (NSCLC) or mesothelioma.[J]. Journal of Clinical Oncology, 2022. DOI:10.1200/jco.2022.40.16_suppl.9071. |
| | APG-2449 Preparation Products And Raw materials |
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