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Home > Products > Specialty & Industrial Chemicals > Specialty Chemicals > AZ 628
AZ 628 structure, CAS 878739-06-1

AZ 628

CAS Number878739-06-1

Synonymscc-82; AZ628; AZ 628

Molecular FormulaC27H25N5O2

Molecular Weight451.52

Purity

Density1.2±0.1 g/cm3

Boiling Point

Melting Point

Flash Point

Appearancewhite to beige

EINECS

MSDSChineseEnglish

Symbol6.1

Signal WordWarning

Cat. No.: 2A-1182953 Purity:
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Quality Control of [ 878739-06-1 ] SDS Specification MoL

COA NMR CNMR HPLC LC-MS
Chemical & Physical Properties
CAS Number878739-06-1
Catalog No.2A-1182953
Chinese Name3-(1-氰基-1-甲基乙基)-N-[3-[(3,4-二氢-3-甲基-4-氧代-6-喹唑啉基)氨基]-4-甲基苯基]苯甲酰胺
Synonymscc-82; AZ628; AZ 628
Molecular FormulaC27H25N5O2
Molecular Weight451.52
Density1.2±0.1 g/cm3
Appearancewhite to beige
Water SolubilityDMSO: soluble10mg/mL, clear
Storage Condition?20°C
ApplicationAZ628 is a pan-Raf kinase inhibitor that inhibits B-Raf, B-RafV600E, and c-Raf-1 with IC50s of 105, 34, and 29 nM, respectively.
HTC2933990090
PubChem ID16780810
SMILESCc1ccc(NC(=O)c2cccc(C(C)(C)C#N)c2)cc1Nc1ccc2ncn(C)c(=O)c2c1
InChIInChI=1S/C27H25N5O2/c1-17-8-9-21(31-25(33)18-6-5-7-19(12-18)27(2,3)15-28)14-24(17)30-20-10-11-23-22(13-20)26(34)32(4)16-29-23/h5-14,16,30H,1-4H3,(H,31,33)
InChI KeyZGBGPEDJXCYQPH-UHFFFAOYSA-N
NACRES CodeNA.77
UNSPSC12352200
Hazard Symbols6.1
BioactivityAZ628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively. Related Catalog Signaling Pathways >> MAPK/ERK Pathway >> Raf Research Areas >> Cancer Target c-Raf-1:29 nM (IC50) B-RafV600E:34 nM (IC50) B-Raf:105 nM (IC50) In Vitro AZ628 reduces activities of preactivated B-Raf, B-RafV600E, and c-Raf-1 in in vitro kinase assays, with IC50 values of 105, 34 and 29 nM, respectively. AZ628 also inhibits activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation[1]. AZ-628 suppresses growth in cells expressing K-RASG13D. Inhibition of RAF with AZ-628 suppresses MEK and ERK phosphorylation. AZ-628 selectively affects viability in K-RAS mutant cells[2]. Cell Assay Cell viability quantified by Syto60 after 72 hours of AZ-628 (0.5, 1.0, and 1.5 μM), CI-1040 or BAY61-3606 treatment in HCT-116 (K-RASG13D/+) or HKe-3 (K-RAS-/+) cell lines. Relative cell viability is normalized to DMSO vehicle treated control for each cell line[2]. References [1]. Khazak V, et al. Selective Raf inhibition in cancer therapy. Expert Opin Ther Targets. 2007 Dec;11(12):1587-609. [2]. Lau KS, et al. BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner. PLoS One. 2012;7(7):e41343. Chemical & Physical Properties Density 1.2±0.1 g/cm3 Molecular Formula C27H25N5O2 Molecular Weight 451.520 Exact Mass 451.200836 PSA 99.81000 LogP 2.78 Appearance of Characters white to beige Index of Refraction 1.638 InChIKey ZGBGPEDJXCYQPH-UHFFFAOYSA-N SMILES Cc1ccc(NC(=O)c2cccc(C(C)(C)C#N)c2)cc1Nc1ccc2ncn(C)c(=O)c2c1 Storage condition ?20°C Water Solubility DMSO: soluble10mg/mL, clear
Use ofAZ628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively. Properties Name 3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxoquinazolin-6-yl)amino]phenyl]benzamide Synonym More Synonyms AZ 628 Biological Activity Description AZ628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively. Related Catalog Signaling Pathways >> MAPK/ERK Pathway >> Raf Research Areas >> Cancer c-Raf-1:29 nM (IC50) B-RafV600E:34 nM (IC50) B-Raf:105 nM (IC50) In Vitro AZ628 reduces activities of preactivated B-Raf, B-RafV600E, and c-Raf-1 in in vitro kinase assays, with IC50 values of 105, 34 and 29 nM, respectively. AZ628 also inhibits activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation[1]. AZ-628 suppresses growth in cells expressing K-RASG13D. Inhibition of RAF with AZ-628 suppresses MEK and ERK phosphorylation. AZ-628 selectively affects viability in K-RAS mutant cells[2]. Cell Assay Cell viability quantified by Syto60 after 72 hours of AZ-628 (0.5, 1.0, and 1.5 μM), CI-1040 or BAY61-3606 treatment in HCT-116 (K-RASG13D/+) or HKe-3 (K-RAS-/+) cell lines. Relative cell viability is normalized to DMSO vehicle treated control for each cell line[2]. References [1]. Khazak V, et al. Selective Raf inhibition in cancer therapy. Expert Opin Ther Targets. 2007 Dec;11(12):1587-609. [2]. Lau KS, et al. BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner. PLoS One. 2012;7(7):e41343. Chemical & Physical Properties Molecular Formula C27H25N5O2 Exact Mass 451.200836 PSA 99.81000 Appearance of Characters white to beige Index of Refraction 1.638 InChIKey ZGBGPEDJXCYQPH-UHFFFAOYSA-N
Tax Rebate13.0%
SupervisionNone. MFN tariff: 6.5%. Ordinary tariff: 20.0%
Transport InfoShipping Name: UN
MSDS Transport InfoModule 14. Shipping information 14.1 UN dangerous goods number European Dangerous Regulations for land transport: 2811 International Dangerous Regulations for sea transport: 2811 International Dangerous Regulations for air transport: 2811 14.2 United Nations shipping name European Land Transport Dangerous Regulations: TOXIC SOLID, ORGANIC, N.O.S. (3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl- 4-oxo-6-quinazolinyl)amino]-4-methylphenyl]-benzamide) IMDG: TOXIC SOLID, ORGANIC, N.O.S. (3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl- 4-oxo-6-quinazolinyl)amino]-4-methylphenyl]-benzamide) International air transport hazard regulations: Toxic solid, organic, n.o.s. (3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6- quinazolinyl)amino]-4-methylphenyl]-benzamide) 14.3 Transport hazard categories European Land Transport Danger Regulations: 6.1 International Maritime Transport Danger Regulations: 6.1 International Air Transport Danger Regulations: 6.1 14.4 Package group European Land Transport Danger Regulations: III International Maritime Transport Danger Regulations: III International Air Transport Danger Regulations: III 14.5 Environmental hazards European Land Transport Danger Regulations: No International Maritime Danger Regulations International Air Transport Danger Regulations: No Marine pollutants (yes/no): No 14.6 Special reminder to users No data available
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