AZ 628
- Product Name
- 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
- Formula Weight
- 451.52
- MOL File
- 878739-06-1.mol
AZ 628 Property
- Density
- 1.21±0.1 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- DMSO: soluble10mg/mL, clear
- pka
- 12.92±0.70(Predicted)
- form
- powder
- color
- white to beige
Safety
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML0785
- Product name
- AZ628
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $73.8
- Updated
- 2024/03/01
- Product number
- SML0785
- Product name
- AZ628
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $482
- Updated
- 2024/03/01
- Product number
- 15336
- Product name
- AZ 628
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 15336
- Product name
- AZ 628
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $93
- Updated
- 2024/03/01
- Product number
- 15336
- Product name
- AZ 628
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
AZ 628 Chemical Properties,Usage,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) | 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
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View Lastest Price from AZ 628 manufacturers
- Product
- AZ 628 878739-06-1
- Price
- US $0.00-0.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 1Ton
- Release date
- 2022-10-13