2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
Description In vitro In vivo- Product Name
- 2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
- CAS No.
- 371242-69-2
- Chemical Name
- 2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
- Synonyms
- CS-428;IC-87114;IC-87114 100MG;IC-87114, >=98%;IC-87114 (PIK-293);IC-87114 (IC87114);IC-87114;IC87114;IC 87114;IC87114 (PI3-K delta inhibitor);2-((6-AMINO-9H-PURIN-9-YL)METHYL)-5-METHYL-3-O-TOLYLQUINAZOLIN-4(3H)-ONE;2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
- CBNumber
- CB12485097
- Molecular Formula
- C22H19N7O
- Formula Weight
- 397.43
- MOL File
- 371242-69-2.mol
2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone Property
- Boiling point:
- 673.7±65.0 °C(Predicted)
- Density
- 1.43
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; insoluble in EtOH; ≥6.62 mg/mL in DMF
- form
- White powder solid.
- pka
- 3.90±0.10(Predicted)
- CAS DataBase Reference
- 371242-69-2
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 11589
- Product name
- IC-87114
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 11589
- Product name
- IC-87114
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $97
- Updated
- 2024/03/01
- Product number
- 11589
- Product name
- IC-87114
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $172
- Updated
- 2024/03/01
- Product number
- 11589
- Product name
- IC-87114
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $745
- Updated
- 2024/03/01
- Product number
- 474112
- Product name
- IC-87114
- Packaging
- 100mg
- Price
- $1507
- Updated
- 2021/12/16
2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone Chemical Properties,Usage,Production
Description
IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β.
In vitro
IC-87114 selectively inhibits PI3Kδ and not sensitive to PI3Kα, β, and γ. In human neutrophils, IC87114 (5 µM) potently inhibits N-formyl-methionyl-leucyl-phenylalanine (fMLP)-stimulated phosphatidylinositol triphosphate (PIP3) biosynthesis and chemotaxis. IC87114 (5 µM) also inhibits polarized morphology and spreading of neutrophils. In human acute myeloid leukemia (AML) blast cells, such as bone marrow mononuclear cells (BMMCs), IC87114 (10 µM) inhibits both constitutive and Flt-3-stimulated Akt phosphorylation and cell proliferation. It is also found that IC87114 (5 µM–30 µM) inhibits SCF-or IL-3-stimulated BMMC responses, which are not observed in PI3Kδ mutant (p110δD910A) cells. In anti-CD3-stimulated mice CD62L+ (naive) and CD62L− (effector/memory) CD4+ T cells, IC87114 inhibits proliferation and interferon-gamma (IFN-γ) production. The IC50 values of IC87114 are: (1) 1.2 µM and 40 nM, for CD62L+ and CD62L− cell proliferation, respectively; (2) 120 nM and 1 nM, for IFN-γ production of CD62L+ and CD62L− cells, respectively. Similar effects by IC87114 are also observed in human T cells. A recent study reveals that in chromaffin cells, IC87114 enhances the transient increase of PtdIns(4,5)P2, which results in a potentiation of exocytosis.
In vivo
In mice, IC87114 (15 mg/kg–60 mg/kg) inhibits the allergic response in the back skin and ear. In mice induced with anti-CD3 or ConA, IC87114 (30 mg/kg) reduces hypersensitivity responses and decreases plasma levels of cytokines, such as IL-2, IL-4, IL-17, IFN-γ, and tumor necrosis factor-α (TNF-α).
Description
The phosphatidylinositol 3-
Uses
IC 87114 is a selective PI3Kδ inhibitor.
Definition
ChEBI: A member of the class of quinazolines that is quinazolin-4(3H)-one carrying (6-amino-9H-purin-9-yl)methyl, 2-methylphenyl and methyl substituents at positions 2, 3 and 5 respectively.
target
PI3Kδ
References
[1]. workman p, van montfort rl. pi(3) kinases: revealing the delta lady. nat chem biol. 2010 feb;6(2):82-3.
[2]. puri kd, doggett ta, douangpanya j, hou y, tino wt, wilson t, graf t, clayton e, turner m, hayflick js, diacovo tg. mechanisms and implications of phosphoinositide 3-kinase delta in promoting neutrophil trafficking into inflamed tissue. blood. 2004 may 1;103(9):3448-56.
[3]. soond dr, bjørgo e, moltu k, dale vq, patton dt, torgersen km, galleway f, twomey b, clark j, gaston js, taskén k, bunyard p, okkenhaug k. pi3k p110delta regulates t-cell cytokine production during primary and secondary immune responses in mice and humans. blood. 2010 mar 18;115(11):2203-13.
2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from 2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone manufacturers
- Product
- 2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone 371242-69-2
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-12-24