AZ 628
- CAS No.
- 878739-06-1
- Chemical Name:
- AZ 628
- Synonyms
- CS-70;AZ-628;AZD628;AZ628, >=99%;AZ628/AZ-628;cas 878739-06-1;AZ-628;CAS 878739-06-1;AZ 628;AZ628;az628 DISCONTINUED, duplicate of A807000;AZ 628,Raf,inhibit,Inhibitor,AZ-628,AZ628,Raf kinases,Apoptosis;3-(2-Cyanopropan-2-yl)-N-(4-methyl-3-((3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino)phenyl)
- CBNumber:
- CB22516246
- Molecular Formula:
- C27H25N5O2
- Molecular Weight:
- 451.52
- MDL Number:
- MFCD17392577
- MOL File:
- 878739-06-1.mol
- MSDS File:
- SDS
Density | 1.21±0.1 g/cm3(Predicted) |
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storage temp. | -20°C |
solubility | DMSO: soluble10mg/mL, clear |
form | powder |
pka | 12.92±0.70(Predicted) |
color | white to beige |
FDA UNII | 560S6B5D79 |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS06 |
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Signal word | Danger | |||||||||
Hazard statements | H301-H315-H319-H335 | |||||||||
Precautionary statements | P301+P310+P330-P302+P352-P305+P351+P338 | |||||||||
Hazard Codes | T | |||||||||
Risk Statements | 25-36/37/38 | |||||||||
Safety Statements | 26-36/37/39-45 | |||||||||
RIDADR | UN 2811 6.1 / PGIII | |||||||||
WGK Germany | 3 | |||||||||
HS Code | 2922500090 | |||||||||
NFPA 704 |
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AZ 628 price More Price(34)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML0785 | AZ628 ≥98% (HPLC) | 878739-06-1 | 5mg | $73.8 | 2024-03-01 | Buy |
Sigma-Aldrich | SML0785 | AZ628 ≥98% (HPLC) | 878739-06-1 | 25mg | $482 | 2024-03-01 | Buy |
Cayman Chemical | 15336 | AZ 628 ≥98% | 878739-06-1 | 1mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 15336 | AZ 628 ≥98% | 878739-06-1 | 5mg | $93 | 2024-03-01 | Buy |
Cayman Chemical | 15336 | AZ 628 ≥98% | 878739-06-1 | 10mg | $169 | 2024-03-01 | Buy |
AZ 628 Chemical Properties,Uses,Production
Uses
AZ 628 is an inhibitor of B-RAF and B-RAF(V600E)
Definition
ChEBI: 3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxo-6-quinazolinyl)amino]phenyl]benzamide is a member of benzamides.
Biological Activity
az628 is a potent and newly discorvered inhibitor of braf, c-raf-1 and brafv600e with ic50 values of 105 nm, 29 nm and 34 nm, respectively. this compound prevents craf activation through persistently occupying the atp-binding site of raf kinase. specificity profile suggests that az628 also inhibits activation of other tyrosine protein kinases such as ddr2, vegfr2, lyn, flt1, fms and others.raf kinases a family of three serine/threonine-specific protein kinases and participate in the ras-raf-mek-erk signal transduction cascade, also known as the mitogen-activated protein kinase (mapk) cascade. the activation of mapk signaling leads to different cellular response such as cell proliferation, apoptosis and inflammation.az628 has the potent anti-tumor activity. in human colon and melanoma-derived cell line that carries the recurrent v600e activating braf mutation, az628 was shown to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis [1]. az628 may be antiangiogenic due to inhibition of vegfr2 [2].generation of melanoma cell line clones is obtained resistance to the raf kinase inhibitor az628. resistance to az628 is connected with raised levels of the raf downstream effector p-erk1/2. erk1/2 initiation in az628-resistant clones is interceded by mek. supported multiplication of az628-resistant clones is to a great extent autonomous of braf kinase action. az628-resistant clones express elevated craf. survival of az628-safe cells is subject to craf [1].
in vitro
AZ628 inhibits B-Raf, B-Raf AZ628 acts on B-Raf-containing M14 parental cell lines treated with increasing concentrations of AZ628, an effective inhibition of p-ERK1/2 levels was observed. It acts on AZ628-resistant M14 cells and does not inhibit ERK activation. AZ628 acts on NRAS-mutated malignant melanoma cells and effectively reduces ERK activation.
target
Target | Value |
C-Raf-1 (Cell-free assay) td> | 29 nM |
B-Raf (V600E) (Cell-free assay) | 34 nM |
B-Raf (Cell-free assay) | 105 nM |
storage
Store at +4°C
References
1. montagut c, sharma sv, shioda t, mcdermott u, ulman m, ulkus le, et al. elevated craf as a potential mechanism of acquired resistance to braf inhibition in melanoma. cancer res 2008,68:4853-4861.2. khazak v, astsaturov i, serebriiskii ig, golemis ea. selective raf inhibition in cancer therapy. expert opin ther targets 2007,11:1587-1609.
AZ 628 Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
Changzhou PBpharmaceutical R&D Co.,Ltd | 0519-83990708 | info@pbpharm.com | CHINA | 498 | 58 |
Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 47465 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Coresyn Pharmatech Co., Ltd. | +86-571-86626709 +86-18157142896 | cbc@coresyn.com | China | 9991 | 58 |
Henan Aochuang Chemical Co.,Ltd. | +86-0371-63689365 +8618638391208 | sales@aochuangchem.com | China | 9425 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |