AS703026
- CAS No.
- 1236699-92-5
- Chemical Name:
- AS703026
- Synonyms
- 100330;CS-397;CS-2173;AS703026;SAR 245509;PiMasertib;MSC1936369B;AS703026/MSC1936369B;AS703026 (Pimasertib);PiMasertib (AS-703026)
- CBNumber:
- CB92537536
- Molecular Formula:
- C15H15FIN3O3
- Molecular Weight:
- 431.2
- MOL File:
- 1236699-92-5.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/7/2 8:55:41
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H319-H335-H302+H312+H332-H315 |
Precautionary statements | P301+P312-P302+P352-P305+P351+P338 |
HS Code | 2933399990 |
AS703026 Chemical Properties,Uses,Production
Uses
AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor, in human multiple myeloma (MM). AS703026 induces pleiotropic anti-myeloma activity in vitro and in vivo. MEK inhibitors are useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.
Enzyme inhibitor
This novel and orally bioavailable MEK1/2 inhibitor (FW = 431.20 g/mol; CAS 1236699-92-5), also known as (S)-N-(2,3-dihydroxypropyl)-3-((2- fluoro-4-iodophenyl)amino)-isonicotinamide, selectively targets MEK1/2 (noncompetitive, with IC50 values of 5-11 nM). AS703026 reduces the growth and survival of multiple myeloma (MM) cells. It also inhibits cytokine-induced osteoclast differentiation about 10x more potently than AZD6244. Inhibition of proliferation by AS703026 leads to G0-G1 cell cycle arrest, attended by reduction in MAF oncogene expression. AS703026 also induces apoptosis (via Caspase-3) as well as poly(ADP- ribose) polymerase (PARP) cleavage in MM cells, whether in the absence or presence of bone marrow stromal cells (BMSCs). Importantly, AS703026 also sensitizes MM cells to other anti-MM therapies employing dexamethasone, melphalan, lenalidomide, perifosine, bortezomib, or rapamycin. Growth reduction in mice bearing H929 MM xenograft tumors correlates with down-regulated pERK1/2, induced PARP cleavage, and decreased microvasculature. BMSC-induced viability of MM patient cells was similarly blocked within the same dose range.
AS703026 Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32835 | 60 | Inquiry |
career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29899 | 58 | Inquiry |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 | China | 49403 | 58 | Inquiry |
ANHUI WITOP BIOTECH CO., LTD | +8615255079626 | China | 23555 | 58 | Inquiry |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 23430 | 58 | Inquiry |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10522 | 58 | Inquiry |
changzhou huayang technology co., ltd | +8615250961469 | China | 9740 | 58 | Inquiry |