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IRAK4-IN-3

Product Name
IRAK4-IN-3
CAS No.
2196204-23-4
Chemical Name
IRAK4-IN-3
Synonyms
AZ1495;IRAK4-IN-3;AZ1495 ，E2647;AZ1495, 10 mM in DMSO;N-(trans-4-Morpholinocyclohexyl)-5-(tetrahydro-2H-pyran-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine;N-((1r,4r)-4-morpholinocyclohexyl)-5-(tetrahydro-2H-pyran-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine;7H-Pyrrolo[2,3-d]pyrimidin-4-amine, N-[trans-4-(4-morpholinyl)cyclohexyl]-5-(tetrahydro-2H-pyran-4-yl)-;N-((1R,4R)-4-Morpholin-4-ylcyclohexyl)-5-(tetrahydro-2H-pyran-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine;AZ-1495,Interleukin-1 receptor associated kinase,interleukin-1 receptor associated kinase 4 (IRAK4),AZ1495,inhibit,cancer,IL-1R associated kinase,AZ 1495,weak base,IRAK,diffuse large B-cell lymphoma (DLBCL),Inhibitor,interleukin-1 receptor associated kinase 1 (IRAK1)
CBNumber
CB74818343
Molecular Formula
C21H31N5O2
Formula Weight
385.5
MOL File
2196204-23-4.mol
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IRAK4-IN-3 Property

Density 
1.265±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 10 mg/mL (25.94 mM)
form 
Solid
pka
13.07±0.50(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0034227
Product name
AZ1495
Purity
99.83%
Packaging
5mg
Price
$550
Updated
2021/12/16
ChemScene
Product number
CS-0034227
Product name
AZ1495
Purity
99.83%
Packaging
10mg
Price
$850
Updated
2021/12/16
ChemScene
Product number
CS-0034227
Product name
AZ1495
Purity
99.83%
Packaging
25mg
Price
$1750
Updated
2021/12/16
ChemScene
Product number
CS-0034227
Product name
AZ1495
Purity
99.83%
Packaging
50mg
Price
$2750
Updated
2021/12/16
ChemScene
Product number
CS-0034227
Product name
AZ1495
Purity
99.83%
Packaging
100mg
Price
$3950
Updated
2021/12/16
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IRAK4-IN-3 Chemical Properties,Usage,Production

Uses

AZ1495, a weak base, is a potent orally active interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor. AZ1495 has a favorable physicochemical and kinase selectivity for IRAK4 and IRAK1 with IC50 values of 0.005 μM and 0.023 μM, respectively. AZ1495 has IRAK4 inhibition with a Kd value of 0.0007 μM. AZ1495 can be used for the research of diffuse large B-cell lymphoma (DLBCL)[1].

in vivo

AZ1495 (compound 28) (oral, daily, 12.5 mg/kg) leds to tumor regression combination with ibrutinib in an ABC-DLBCL mouse model (OCI-LY10 cells)[1].
AZ1495 (iv., 2 mg/kg and oral, 5mg/kg) is characterized by high clearance (Cl) in rat (75 mL/min/kg) and moderate predictions based on hepatocyte data (Clint 15 μl/min/106 cells, predicted clearance 42 mL/min/kg) with low bioavailability consistent with a high first pass effect[1].
AZ1495 (iv., 1 mg/kg) has low the amount of active renal secretion occurring in the dog[1].

Animal Model:CB.17 SCID mice[1]
Dosage:12.5 mg/kg
Administration:oral, daily, 12.5 mg/kg
Result:Had modest anti-tumor activity as single agents but a combination ofibrutinib led to tumor regression and is well tolerated.
Animal Model:rat[1]
Dosage:2 mg/kg, 5mg/kg
Administration:iv., 2 mg/kg and oral, 5mg/kg
Result:
SpeciesDose (mg/kg)Cl (mL/min/kg)Vss(L/kg)PO halflife (h)IV halflife (h)Fabs (%)F (%)
Rat2，5752.12.00.810028
Dog1293.0-3.3--
Animal Model:dog[1]
Dosage:1 mg/kg
Administration:iv., 1 mg/kg
Result:
SpeciesDose (mg/kg)Cl (mL/min/kg)Vss(L/kg)PO halflife (h)IV halflife (h)Fabs (%)F (%)
Rat2，5752.12.00.810028
Dog1293.0-3.3--

IC 50

IRAK4: 5 nM (IC50); IRAK1: 23 nM (IC50); CLK1: 50 nM (IC50); CLK2: 5 nM (IC50); CLK4: 8 nM (IC50); haspin: 4 nM (IC50)

References

[1] Scott JS, et al. Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma. J Med Chem. 2017 Dec 28;60(24):10071-10091. DOI:10.1021/acs.jmedchem.7b01290

IRAK4-IN-3 Preparation Products And Raw materials

Raw materials

Preparation Products

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IRAK4-IN-3 Suppliers

China 32 United States 5 Global 37
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070 13913916777
Fax
+86-25-83453306
Email
info@chemlin.com.cn
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China
ProdList
16027
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Shanghai Raise Chemical Technology Co.,Ltd
Tel
15026594951
Fax
0556-5030632
Email
rs@raise-chem.com
Country
China
ProdList
4677
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55
Bide Pharmatech Ltd.
Tel
400-400-164-7117 18317119277
Fax
+86-21-61629029
Email
product02@bidepharm.com
Country
China
ProdList
40000
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60
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4817
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55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
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58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
86249
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60
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9729
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58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32467
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58
BOC Sciences
Tel
+1-631-485-4226
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1-631-614-7828
Email
inquiry@bocsci.com
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United States
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19552
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
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sales@chemegen.com
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China
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11218
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2196204-23-4, IRAK4-IN-3Related Search:


  • IRAK4-IN-3
  • AZ1495
  • 7H-Pyrrolo[2,3-d]pyrimidin-4-amine, N-[trans-4-(4-morpholinyl)cyclohexyl]-5-(tetrahydro-2H-pyran-4-yl)-
  • N-(trans-4-Morpholinocyclohexyl)-5-(tetrahydro-2H-pyran-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
  • AZ-1495,Interleukin-1 receptor associated kinase,interleukin-1 receptor associated kinase 4 (IRAK4),AZ1495,inhibit,cancer,IL-1R associated kinase,AZ 1495,weak base,IRAK,diffuse large B-cell lymphoma (DLBCL),Inhibitor,interleukin-1 receptor associated kinase 1 (IRAK1)
  • N-((1r,4r)-4-morpholinocyclohexyl)-5-(tetrahydro-2H-pyran-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
  • AZ1495, 10 mM in DMSO
  • AZ1495 ，E2647
  • N-((1R,4R)-4-Morpholin-4-ylcyclohexyl)-5-(tetrahydro-2H-pyran-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine
  • 2196204-23-4