4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine
- Product Name
- 4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine
- CAS No.
- 6975-75-3
- Chemical Name
- 4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine
- Synonyms
- ILK-IN-3;ILK-IN-3 ，E0790;ILK-IN-3, 10 mM in DMSO;4-[2-(4-Methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine;antitumor,Integrin,inhibit,ILK,Inhibitor,ILK IN 3,ILKIN3;1H-Pyrazole-3,5-diamine, 4-[2-(4-methoxyphenyl)diazenyl]-;4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine;3-amino-4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazol-5-ylamine
- CBNumber
- CB02111670
- Molecular Formula
- C10H12N6O
- Formula Weight
- 232.24
- MOL File
- 6975-75-3.mol
4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine Property
- storage temp.
- Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
- solubility
- DMSO: 83.33 mg/mL (358.81 mM)
- form
- Solid
- color
- Light yellow to yellow
- InChI
- 1S/C10H12N6O/c1-17-7-4-2-6(3-5-7)13-14-8-9(11)15-16-10(8)12/h2-5H,1H3,(H5,11,12,15,16)/b14-13+
- InChIKey
- QNRNTYHAOBVOKW-BUHFOSPRSA-N
- SMILES
- [nH]1nc(c(c1N)\N=N\c2ccc(cc2)OC)N
Safety
- WGK Germany
- WGK 3
- Storage Class
- 11 - Combustible Solids
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H314Causes severe skin burns and eye damage
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P330+P331IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.
P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.
P363Wash contaminated clothing before reuse.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- CS-0104348
- Product name
- ILK-IN-3
- Purity
- 99.57%
- Packaging
- 5mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- 173325
- Product name
- 3-Amino-4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazol-5-ylamine
- Packaging
- 1g
- Price
- $316
- Updated
- 2021/12/16
- Product number
- CS-0104348
- Product name
- ILK-IN-3
- Purity
- 99.57%
- Packaging
- 25mg
- Price
- $700
- Updated
- 2021/12/16
- Product number
- 173325
- Product name
- 3-Amino-4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazol-5-ylamine
- Packaging
- 5g
- Price
- $810
- Updated
- 2021/12/16
- Product number
- 173325
- Product name
- 3-Amino-4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazol-5-ylamine
- Packaging
- 10g
- Price
- $1170
- Updated
- 2021/12/16
4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine Chemical Properties,Usage,Production
Uses
ILK-IN-3 is an orally active integrin linked kinase (ILK) inhibitor. ILK-IN-3 improves the anticancer efficacy of Docetaxel.html" class="link-product" target="_blank">Docetaxel (HY-B0011) in orthotopic LCC6 model[1][2].
Biological Activity
QLT0267 is an orally active, potent and selective integrin-linked kinase (ILK) inhibitor (IC50 = 26 nM; selectivity: >1000-fold over CK2, CSK, DNA-PK, PIM1, PKB/AKT, PKC, >100-fold over ERK1, GSK3β, LCK, PKA, p70S6K, and RSK1/QLT, >10-fold over CDK1/2/5) th at inhibits ILK-dependent cellular signaling (IC50 in 2h = 1 μM against 20 nM EGF-induced pAKT Ser473 phosphorylation in Hth74 cells). QLT0267 treatment causes thyroid cancer cell cycle arrest and apoptosis, leading to anti-proliferation efficacy in cultures (IC50 <6 μM; NPA187, DRO, and K4 cell lines) and in mice in vivo (DRO xenografts-derived tumor growth; 50-100 mg/kg via daily p.o.).
in vivo
ILK-IN-3 (QLT0267) (200 mg/kg; po; 28 days) Inhibits tumor growth in the in situ LCC6 model[1].
IC 50
DYRK1
References
[1] Jessica Kalra, et al. Validating the Use of a Luciferase Labeled Breast Cancer Cell Line, MDA435LCC6, as a Means to Monitor Tumor Progression and to Assess the Therapeutic Activity of an Established Anticancer Drug, Docetaxel (Dt) Alone or in Combination With the ILK Inhibitor, QLT0267. Cancer Biol Ther. 2011 May 1;11(9):826-38. DOI:10.4161/cbt.11.9.15183
[2] Mavrogeni ME, et al. A facile consensus ranking approach enhances virtual screening robustness and identifies a cell-active DYRK1α inhibitor. Future Med Chem. 2018 Oct;10(20):2411-2430. DOI:10.4155/fmc-2018-0198
4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine Preparation Products And Raw materials
Raw materials
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