ChemicalBook > CAS DataBase List > AZD6738

AZD6738

Product Name
AZD6738
CAS No.
1352226-88-0
Chemical Name
AZD6738
Synonyms
CERALASERTIB;(3R)-3-Methyl-4-(6-((2R)-2-((R)-S-methylsulfonimidoyl)cyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin;AZD-6738;AZD6738;CS-1601;EOS-61602;Trilacicli;10G,100G,500G;AZD6738(AZD-6738);AZD6738(Ceralasertib)
CBNumber
CB92747926
Molecular Formula
C20H24N6O2S
Formula Weight
412.51
MOL File
1352226-88-0.mol
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AZD6738 Property

Density 
1.52±0.1 g/cm3(Predicted)
storage temp. 
Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility 
DMSO (Slightly), Methanol (Slightly)
form 
Solid
pka
12.53±0.40(Predicted)
color 
Pale Yellow
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Safety

HS Code 
2934999090
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
21035
Product name
AZD 6738
Purity
≥98%
Packaging
1mg
Price
$49
Updated
2024/03/01
Cayman Chemical
Product number
21035
Product name
AZD 6738
Purity
≥98%
Packaging
5mg
Price
$216
Updated
2024/03/01
Cayman Chemical
Product number
21035
Product name
AZD 6738
Purity
≥98%
Packaging
10mg
Price
$380
Updated
2024/03/01
Cayman Chemical
Product number
21035
Product name
AZD 6738
Purity
≥98%
Packaging
25mg
Price
$830
Updated
2024/03/01
TRC
Product number
A965423
Product name
AZD6738
Packaging
1mg
Price
$45
Updated
2021/12/16
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AZD6738 Chemical Properties,Usage,Production

Description

AZD 6738 is an orally bioavailable inhibitor of the serine/threonine protein kinase ataxia telangiectasia mutated (ATM) and Rad3-related (ATR; IC50 = 1 nM). It can inhibit ATR substrate Chk1 Ser345 phosphorylation in cells with an IC50 value of 74 nM. AZD 6738 has been shown to inhibit the proliferation of various solid and hematological cell lines with IC50 values of less than 1 μM and to reduce tumor growth in several ATM-deficient xenograft models. When used in combination with either DNA damaging chemotherapy agents or ionizing radiation, AZD 6738 demonstrated synergistic cell killing activity across multiple cell lines in vitro and in xenograft studies.

Uses

AZD6738 is an orally available morpholino-pyrimidine-based inhibitor of ataxia telangiectasia and rad3 related (ATR) kinase, with potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor AZD6738 selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-mediated signaling, and results in the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis. In addition, AZD6738 sensitizes tumor cells to chemo- and radiotherapy. ATR, a serine/threonine protein kinase upregulated in a variety of cancer cell types, plays a key role in DNA repair, cell cycle progression, and survival; it is activated by DNA damage caused during DNA r

Enzyme inhibitor

This orally active, and selective ATR kinase inhibitor (FW = 412.51 g/mol; CAS 1352226-88-0; Solubility: 80 mg/mL DMSO; < 1 mg/mL H2O) targets Ataxia Telangiectasia/Rad3-related kinase (IC50 = 1 nM), a serine/threonine protein kinase that activates checkpoint signaling upon genotoxic stresses (e.g., ionizing radiation, ultraviolet light, or replication stalling), thereby serving as a DNA damage sensor. In a model consisting of primary human Chronic Myelogenous Leukemia (CL) cells with biallelic TP53 or ATM inactivation xenotransplanted into NOD/Shi scid/IL-2Rγ mice, AZD6738 provides potent and specific inhibition of ATR signalling with compensatory activation of ATM/p53 pathway in cycling CLL cells in the presence of genotoxic stress. In p53 or ATM defective cells, AZD6738 treatment results in replication fork stalls and accumulation of unrepaired DNA damage, as evidenced by γH2AX and 53BP1 foci formation, carried through into mitosis and resulting in cell death by mitotic catastrophe. AZD6738 displays selective cytotoxicity towards ATM- or p53-deficient CLL cells. AZD6738 also potentiates cisplatin and gemcitabine cytotoxicity in Non-Small-Cell Lung Carcinoma (NSCLC) cell lines with intact ATM kinase signaling. It also potently synergizes with cisplatin in ATM-deficient NSCLC cells. When used in combination, cisplatin and AZD6738 resolve ATM-deficient lung cancer xenografts.

References

[1]. choi my, fecteau jf, brown j, et al. induction of proliferation sensitizes chronic lymphocytic leukemia cells to apoptosis mediated by the atr inhibitor azd6738. cancer research, 2014, 74(19 supplement): 5485-5485.
[2]. checkley s, maccallum l, yates j, et al. bridging the gap between in vitro and in vivo: dose and schedule predictions for the atr inhibitor azd6738. scientific reports, 2015, 5.
[3]. guichard sm, brown e, odedra r, et al. the pre-clinical in vitro and in vivo activity of azd6738: a potent and selective inhibitor of atr kinase. cancer research, 2013, 73(8 supplement): 3343-3343.

AZD6738 Preparation Products And Raw materials

Raw materials

Preparation Products

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AZD6738 Suppliers

China 121 India 1 United States 10 Global 132
Changzhou Chenhong Biotechnology Co., Ltd.
Tel
0519-85788828 13775037613
Email
sales@chemrenpharm.com
Country
China
ProdList
3553
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4121
Advantage
55
Wuhan Shanhai Zhihe Biotechnology Co., Ltd.
Tel
17771424646
Email
shoubull@126.com
Country
China
ProdList
965
Advantage
58
Wuhan Jingkangen Biomedical Technology Co., Ltd
Tel
13720134139 13720134139
Email
orders@jknbiochem.com
Country
China
ProdList
4958
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2923
Advantage
55
Chembest Research Laboratories Limited
Tel
021-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6011
Advantage
61
BeiJing Hwrk Chemicals Limted
Tel
0757-86329057 18501085097
Fax
010-89508210
Email
sales3.gd@hwrkchemical.com
Country
China
ProdList
7639
Advantage
55
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4647
Advantage
58
T&W GROUP
Tel
021-61551611 13296011611
Fax
＋86 21-50676805
Email
contact@trustwe.com
Country
China
ProdList
9900
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7553
Advantage
61
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View Lastest Price from AZD6738 manufacturers

Honest Joy Holdings Limited
Product
AZD6738 1352226-88-0
Price
US $0.00/KG
Min. Order
1KG
Purity
99.1%
Supply Ability
100 tons
Release date
2022-01-13
Career Henan Chemical Co
Product
AZD6738 1352226-88-0
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-23

1352226-88-0, AZD6738Related Search:

SGC707 MS023 3,4-dimethoxy-N-[4-(3-nitrophenyl)-1,3-thiazol-2-yl]benzenesulfonamide indoleaMine-2,3-dioxygenase inhibitor INCB024360 LLY-507 4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide DBeQ BLU 9931 2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione Enasidenib RVX-208 Epacadostat (INCB024360)

  • AZD6738
  • AZD-6738
  • 4-[4-[1-[[S(R)]-S-Methylsulfonimidoyl]cyclopropyl]-6-[(3R)-3-methyl-4-morpholinyl]-2-pyrimidinyl]-1H-pyrrolo[2,3-b]pyridine
  • AZD6738(AZD-6738)
  • EOS-61602
  • (R)-3-methyl-4-(6-(1-((R)-S-methylsulfonimidoyl)cyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl)morpholine
  • 1H-Pyrrolo[2,3-b]pyridine, 4-[4-[1-[[S(R)]-S-methylsulfonimidoyl]cyclopropyl]-6-[(3R)-3-methyl-4-morpholinyl]-2-pyrimidinyl]-
  • (R)-imino(methyl)(1-(6-((R)-3-methylmorpholino)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl)cyclopropyl)-l6-sulfanone
  • (3R)-3-Methyl-4-(6-((2R)-2-((R)-S-methylsulfonimidoyl)cyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin
  • CERALASERTIB
  • AZD-6738;AZD 6738;AZD6738
  • (R)-imino(methyl)(1-(6-((R)-3-methylmorpholino)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl)cyclopropyl)-l6-sulfanone (AZD6738)
  • CS-1601
  • AZD6738， Ceralasertib, M6620
  • CERALASERTIB (AZD6738)
  • 10G,100G,500G
  • Trilacicli
  • (3R)-3-Methyl-4-(6-((2R)-2-((R)-S-methylsulfonimidoyl)cyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl)morpholine
  • (R)-3-Methyl-4-[6-[1-[(R)-S-methylsulfonimidoyl]cyclopropyl]-2-(7-azaindol-4-yl)-4-pyrimidinyl]morpholine
  • AZD6738(Ceralasertib)
  • 1352226-88-0