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AZD 5438

Product Name
AZD 5438
CAS No.
602306-29-6
Chemical Name
AZD 5438
Synonyms
AZD;CS-1903;AZD 5438;AZD5438, >=98%;AZD5438 ，S2621;AZD 5438; AZD5438;AZD 5438 USP/EP/BP;AZD5438 >=97% (HPLC);AZD-5438, 10 mM in DMSO;4-[2-Methyl-1-(1-Methylethyl)-1H-iMidazol-5-yl]-N-[4-(Methylsulfonyl)phenyl]-
CBNumber
CB61512498
Molecular Formula
C18H21N5O2S
Formula Weight
371.46
MOL File
602306-29-6.mol
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AZD 5438 Property

Boiling point:
655.2±65.0 °C(Predicted)
Density 
1.31
storage temp. 
Keep in dark place,Inert atmosphere,2-8°C
solubility 
insoluble in H2O; ≥18.55 mg/mL in DMSO; ≥42.1 mg/mL in EtOH
form 
solid
pka
4.08±0.50(Predicted)
color 
White to light yellow
InChI
InChI=1S/C18H21N5O2S/c1-12(2)23-13(3)20-11-17(23)16-9-10-19-18(22-16)21-14-5-7-15(8-6-14)26(4,24)25/h5-12H,1-4H3,(H,19,21,22)
InChIKey
WJRRGYBTGDJBFX-UHFFFAOYSA-N
SMILES
C1(NC2=CC=C(S(C)(=O)=O)C=C2)=NC=CC(C2N(C(C)C)C(C)=NC=2)=N1
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H401Toxic to aquatic life

Precautionary statements

P273Avoid release to the environment.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1855
Product name
AZD5438
Purity
≥97% (HPLC)
Packaging
5MG
Price
$101.7
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1855
Product name
AZD5438
Purity
≥97% (HPLC)
Packaging
25MG
Price
$436
Updated
2025/07/31
Cayman Chemical
Product number
21598
Product name
AZD 5438
Purity
≥98%
Packaging
5mg
Price
$89
Updated
2024/03/01
Cayman Chemical
Product number
21598
Product name
AZD 5438
Purity
≥98%
Packaging
10mg
Price
$168
Updated
2024/03/01
Cayman Chemical
Product number
21598
Product name
AZD 5438
Purity
≥98%
Packaging
25mg
Price
$374
Updated
2024/03/01
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AZD 5438 Chemical Properties,Usage,Production

Uses

AZD 5438 is a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, which leads to leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts.

Definition

ChEBI: 4-(2-methyl-3-propan-2-yl-4-imidazolyl)-N-(4-methylsulfonylphenyl)-2-pyrimidinamine is a sulfonamide.

Biological Activity

azd5438 is a potent small molecule inhibitor of cyclin-dependent kinase (cdk) 1, 2 and 9 with half maximal inhibitory concentration ic50 of 16 nmol/l, 6 nmol/l and 20 nmol/l respectively. azd5438 has also been found to potently inhibit the human cyclin e/cdk2 complex, the cyclin b1/cdk1 complex and the cyclin a/cdk2 complex with ic50 of 0.006 μm, 0.016 μm and 0.045 μm respectively. in previous studies, azd5438 has exhibited significant anti-proliferative activity in a few human tumor cell lines with ic50 ranging from 0.2 μmol/l to 1.7 μmol/l, in which the phosphorylation of a few proteins, including cdk substrates prb, nucleolin, protein phosphatase 1a and rna polymerase ii cooh-terminal domain, and cell cycling at g2-m, s and g1 phases were inhibited.

in vivo

AZD5438 (50 mg/kg twice daily or 75 mg/kg, p.o.) inhibits human tumor xenograft growth. In vivo, AZD5438 reduces the proportion of actively cycling cells. Further pharmacodynamic analysis of AZD5438-treated SW620 xenografts shows that efficacious doses of AZD5438 (>40% tumor growth inhibition) maintains suppression of biomarkers, such as phospho-pRbSer249/Thr252, for up to 16 hours following a single oral dose[1].

IC 50

cdk2-cyclin E: 6 nM (IC50); cdk2-cyclin A: 45 nM (IC50); cdk5-p25: 14 nM (IC50); cdk1-cyclin B1: 16 nM (IC50); cdk9-cyclin T: 20 nM (IC50); cdk6-cyclin D3: 21 nM (IC50); cdk4-cyclin D1: 449 nM (IC50); cdk7-cyclin H: 821 nM (IC50)

storage

Desiccate at RT

References

[1]camidge dr1, smethurst d, growcott j, barrass nc, foster jr, febbraro s, swaisland h, hughes a. a first-in-man phase i tolerability and pharmacokinetic study of the cyclin-dependent kinase-inhibitor azd5438 in healthy male volunteers. cancer chemother pharmacol. 2007 aug;60(3):391-8. epub 2006 nov 18.
[2]byth kf, thomas a, hughes g, forder c, mcgregor a, geh c, oakes s, green c, walker m, newcombe n, green s, growcott j, barker a, wilkinson rw. azd5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. mol cancer ther. 2009 jul;8(7):1856-66. doi: 10.1158/1535-7163.mct-08-0836. epub 2009 jun 9.

AZD 5438 Preparation Products And Raw materials

Raw materials

Preparation Products

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AZD 5438 Suppliers

China 154 India 1 United Kingdom 2 United States 20 Global 177
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15838
Advantage
69
ChemFuture PharmaTech (Jiangsu) Ltd
Tel
5108538618
Fax
86 510 85386988-8017
Email
suger.wang@chemfuture.com
Country
China
ProdList
832
Advantage
65
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
Advantage
61
Capot Chemical Co., Ltd
Tel
+86 (0) 571 85 58 67 18
Fax
0086-571-85864795
Country
China
ProdList
18207
Advantage
66
JinYan Chemicals(ShangHai) Co.,Ltd.
Tel
13817811078
Fax
86-021-50426522,50426273
Email
sales@jingyan-chemical.com
Country
China
ProdList
9976
Advantage
60
Pure Chemistry Scientific Inc.
Tel
001-857-928-2050 or 1-888-588-9418
Fax
001-617-206-9595
Email
sales@chemreagents.com
Country
United States
ProdList
10186
Advantage
62
VDM Biochemicals
Tel
0330-2528181
Fax
0330-2528171
Email
sales@vdmbio.com
Country
United States
ProdList
510
Advantage
64
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com
Country
China
ProdList
1856
Advantage
62
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View Lastest Price from AZD 5438 manufacturers

HangZhou RunYan Pharma Technology Co.,LTD.
Product
AZD-5438；AZD5438 602306-29-6
Price
US $0.00-0.00/g
Min. Order
10g
Purity
99.0%min. HPLC
Supply Ability
1000kg
Release date
2024-11-23
Career Henan Chemical Co
Product
AZD 5438 602306-29-6
Price
US $9.80/KG
Min. Order
1g
Purity
≥99%
Supply Ability
100kg
Release date
2019-12-25

602306-29-6, AZD 5438Related Search:

p-Menthane 4-METHYL-2-PENTYNE Cumene Alisertib (MLN8237) BMS-265246 PD 0332991 HCl (2S)-1-[3-Ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2-piperidineethanol Flavopiridol (Alvocidib) HCl Olaparib 1-ISOPROPYL-2,5-DIMETHYLIMIDAZOLE AZD 5438

  • 2-Pyrimidinamine,4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-
  • AZD 5438
  • 4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine
  • AZD
  • 4-[2-Methyl-1-(1-Methylethyl)-1H-iMidazol-5-yl]-N-[4-(Methylsulfonyl)phenyl]-
  • 2-Pyrimidinamine,4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-(AZD 5438)
  • 4-[2-Methyl-1-isopropyl-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine
  • 4-[2-Methyl-1-isopropyl-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine AZD 5438
  • AZD 5438 4-[2-Methyl-1-isopropyl-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine
  • AZD5438, >=98%
  • CS-1903
  • AZD 5438; AZD5438
  • AZD5438 >=97% (HPLC)
  • AZD 5438 USP/EP/BP
  • AZD-5438, 10 mM in DMSO
  • AZD5438 ，S2621
  • 602306-29-6
  • C18H21N5O2S
  • Inhibitors
  • API intermediates
  • Potent inhibitor of cyclin-dependent kinase (cdk) 1, 2 and 9.