ATM-ATR-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/ATM_ATR.html ATM/ATRAtaxia telangiectasia mutated; ATM and RAD3 relatedATM/ATR, members of the phosphatidyl inositol 3-kinase-like family of serine/threonine protein kinases (PIKKs), are widely knownas being central players in the mitotic DNA damage response (D

2、DR), mounting responses to DNA double-strand breaks (DSBs) andsingle-stranded DNA (ssDNA) respectively. Activation of ATM by ionizing radiation results in the activation of signal transductionpathways that induce cell cycle arrest at G1/S, S and G2/M. ATR is required for cell cycle arrest in respons

3、e to DNA-damagingagents such as ultraviolet radiation that cause bulky lesions.Upon activation, ATM/ATR phosphorylate numerous targets to stabilize stalled replication forks, repair damaged DNA, and inhibitcell cycle progression to ensure survival of the cell and safeguard integrity of the genome. A

4、TM and ATR are central players inactivating cell cycle checkpoints and function as an active barrier against genome instability and tumorigenesis in replicating cells.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/ATM/ATR.html ATM/ATR HYPERLINK https:/www.MedChemE/Targets/ATM/ATR.html HYPERLIN

5、K https:/www.MedChemE/Targets/ATM/ATR.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/ATM/ATR.html HYPERLINK https:/www.MedChemE/Targets/ATM/ATR.html & HYPERLINK https:/www.MedChemE/Targets/ATM/ATR.html HYPERLINK https:/www.MedChemE/Targets/ATM/ATR.html Activators HYPERLINK https:/www.MedChemE

6、/s-ceralasertib.html (S)-Ceralasertib(S)-AZD6738) Cat. No.: HY-19323A HYPERLINK https:/www.MedChemE/antitumor-agent-28.html Antitumor HYPERLINK https:/www.MedChemE/antitumor-agent-28.html HYPERLINK https:/www.MedChemE/antitumor-agent-28.html agent-28Cat. No.: HY-141478(S)-Ceralasertib (S)-AZD6738) i

7、s extracted frompatent WO2011154737A1, Compound II, exhibits anIC of 2.578 nM.50Antitumor agent-28 selectively inhibits ataxiatelangiectasia mutated (ATM) kinase. Antitumoragent-28 prevents ATM mediated disease and haspotent anti-cancer activity.Purity: 95.66%Clinical Data:Size: 10 mM 1 mL, 5 mg, 10

8、 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ATM_Inhibitor-1.html ATM HYPERLINK https:/www.MedChemE/ATM_Inhibitor-1.html HYPERLINK https:/www.MedChemE/ATM_Inhibitor-1.html Inhibitor-1 HYPERLINK https:/www.MedChemE/ATM_Inhibitor-1.h

9、tml HYPERLINK https:/www.MedChemE/atm-inhibitor-2.html ATM HYPERLINK https:/www.MedChemE/atm-inhibitor-2.html HYPERLINK https:/www.MedChemE/atm-inhibitor-2.html Inhibitor-2Cat. No.: HY-112614 Cat. No.: HY-144685ATM Inhibitor-1 is a highly potent, selective andorally active ATM inhibitor, with an IC

10、of500.7 nM, shows weak activity against mTOR (IC , 2150M), DNAPK (IC , 2.8 M), PI3K (IC , 3.8 M),50 50PI3K (IC , 10.3 M), PI3K (IC , 3 M) and PI3K50 50(IC , 0.73 M).50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgATM Inhibitor-2 (compound 7) is a potent andselective ATM inhibitor,

11、 with an IC of 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/atm-inhibitor-3.html ATM HYPERLINK https:/www.MedChemE/atm-inhibitor-3.html HYPERLINK https:/www.MedChemE/atm-inhibitor-3.html Inhibitor-3 HYPERLINK https:/www.MedChemE/atm-inhibitor-3.html HYPERLI

12、NK https:/www.MedChemE/atm-inhibitor-4.html ATM HYPERLINK https:/www.MedChemE/atm-inhibitor-4.html HYPERLINK https:/www.MedChemE/atm-inhibitor-4.html Inhibitor-4Cat. No.: HY-144686 Cat. No.: HY-144687ATM Inhibitor-3 (compound 34) is a potent andselective ATM inhibitor, with an IC of 0.7150nM. ATM In

13、hibitor-3 shows inhibition of PI3Kkinases family. ATM Inhibitor-3 exhibits favorablemetabolic stability.ATM Inhibitor-4 (compound 39) is a potent andselective ATM inhibitor, with an IC of 0.3250nM. ATM Inhibitor-4 shows stronger inhibition ofPI3K kinases family. ATM Inhibitor-4 shows a fullinhibitio

14、n of mTOR at 1 M. ATM Inhibitor-4exhibits favorable metabolic stability.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/atm-in-1.html ATM-IN-1 HYPERLINK https:/www.MedChemE/atm-in-1.html

15、HYPERLINK https:/www.MedChemE/atr-inhibitor-1.html ATR HYPERLINK https:/www.MedChemE/atr-inhibitor-1.html HYPERLINK https:/www.MedChemE/atr-inhibitor-1.html inhibitor HYPERLINK https:/www.MedChemE/atr-inhibitor-1.html HYPERLINK https:/www.MedChemE/atr-inhibitor-1.html 1Cat. No.: HY-142931 Cat. No.:

16、HY-111451ATM-IN-1 is a potent inhibitor of ATM. ATM islocated mainly in the nucleus and microsomes andis involved in cell cycle progression and in thecell cycle checkpoint response to DNA damage.ATR inhibitor 1 is a ATR inhibitor extracted frompatent WO2015187451A1, compound I-l, has a Kvalue below

17、1 .iPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/atr-in-10.html ATR-IN-10 HYPERLINK https:/www.MedChemE/atr-in-10.html HYPERLINK https:/www.MedChemE/atr-in-11.ht

18、ml ATR-IN-11Cat. No.: HY-144214 Cat. No.: HY-144435ATR-IN-10 is a potent and highly selectiveinhibitor of ataxia telangiectasia mutated andRad3-Related (ATR) kinase with an IC value of502.978 M.ATR-IN-11 (Compound Hit01) is a potent inhibitorof ataxia telangiectasia and Rad3-related (ATR)kinase. ATR

19、 kinase is a key regulating proteinwithin the DNA damage response (DDR), responsiblefor sensing replication stress (RS).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: sales

20、MedChemE HYPERLINK https:/www.MedChemE/atr-in-12.html ATR-IN-12 HYPERLINK https:/www.MedChemE/atr-in-12.html HYPERLINK https:/www.MedChemE/atr-in-13.html ATR-IN-13Cat. No.: HY-144436 Cat. No.: HY-147565ATR-IN-12 (Compound 5g) is a potent inhibitor ofataxia telangiectasia and Rad3-related (ATR)kinase

21、 with an IC value of 0.007 M.50ATR-IN-13 (compound A9) is a potent ATR kinaseinhibitor, with an IC of 2 nM. ATR-IN-13 can be50used for ATR kinase mediated diseases research,such as proliferative diseases and cancer.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical

22、Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/atr-in-14.html ATR-IN-14 HYPERLINK https:/www.MedChemE/atr-in-14.html HYPERLINK https:/www.MedChemE/atr-in-15.html ATR-IN-15Cat. No.: HY-147566 Cat. No.: HY-147567ATR-IN-14 (compound 1) is a potent ATR kinaseinhibitor. ATR-I

23、N-14 inhibits ATR signalingpathways downstream CHKI protein phosphorylation,with inhibition of 98.03% at 25 nM. ATR-IN-14shows good anticancer activity in LoVo cells, withan IC of 64 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgATR-IN-15 (compound 1) is an orally active andp

24、otent ATR kinase inhibitor, with an IC of 850nM. ATR-IN-15 also inhibits human colon tumorcells LoVo, DNA-PK and PI3K, with IC values of5047, 663 and 5131 nM, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/atr-in-16.html ATR-IN-16 HYPERLI

25、NK https:/www.MedChemE/atr-in-16.html HYPERLINK https:/www.MedChemE/atr-in-17.html ATR-IN-17Cat. No.: HY-147568 Cat. No.: HY-147569ATR-IN-16 (compound 46) is a potent ATR kinaseinhibitor. ATR-IN-16 shows good anticanceractivity in LoVo cells, with an IC of 410 nM.50ATR-IN-17 (compound 88) is a poten

26、t ATR kinaseinhibitor. ATR-IN-17 shows good anticanceractivity in LoVo cells, with an IC of 1 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/atr-in-18.html ATR-IN-18 HYPERLINK https

27、:/www.MedChemE/atr-in-18.html HYPERLINK https:/www.MedChemE/atr-in-4.html ATR-IN-4Cat. No.: HY-147570 Cat. No.: HY-145312ATR-IN-18 (compound 2) is an orally active andpotent ATR kinase inhibitor, with an IC of 0.6950nM. ATR-IN-18 shows antiproliferative activity inLoVo cells, with an IC of 37.34 nM.

28、 ATR-IN-1850has anti-tumor activity.ATR-IN-4 is a potent ATR (Ataxia telangiectasiamutated gene Rad 3-associated kinase) inhibitor.ATR-IN-4 inhibits growth of human prostate cancercells DU145 and human lung cancer cells NCI-H460with IC s of 130.9 nM and 41 .33 nM, respectively.50(Patent CN112142744A

29、, compound 13).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/atr-in-5.html ATR-IN-5 HYPERLINK https:/www.MedChemE/atr-in-5.html HYPERLINK https:/www.MedChemE/atr-in-6.html ATR-IN-6Cat.

30、No.: HY-142671 Cat. No.: HY-142672ATR-IN-5 is a potent inhibitor of ATR. ATR is aclass of protein kinases involved in genomestability and DNA damage repair, and is a memberof the PIKK family.ATR-IN-6 is a potent inhibitor of ATR. ATR is aclass of protein kinases involved in genomestability and DNA d

31、amage repair, and is a memberof the PIKK family.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/atr-in-7.html ATR-IN-7 HYPERLINK https:/www.MedChemE/atr-in-7.html HYPERLINK

32、https:/www.MedChemE/atr-in-8.html ATR-IN-8Cat. No.: HY-142673 Cat. No.: HY-142924ATR-IN-7 is a potent inhibitor of ATR. ATR is aclass of protein kinases involved in genomestability and DNA damage repair, and is a memberof the PIKK family.ATR-IN-8 is a potent inhibitor of ATR. ATR is akey enzyme in t

33、he homologous recombination repairpathway and belongs to the PIKK family. ATR-IN-8has the potential for the research of cancerdiseases (extracted from patent WO2021143821A1,compound 3).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedS

34、ize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AZ20.html AZ20 HYPERLINK https:/www.MedChemE/AZ20.html HYPERLINK https:/www.MedChemE/AZ32.html AZ32Cat. No.: HY-15557 Cat. No.: HY-112305AZ20 is a potent and selective inhibitor of ATRwith an IC of 5 nM, and has 8-fold selectivity50against mTOR (IC =38 n

35、M).50AZ32 is an orally bioavailable and blood-brainbarrier-penetrating ATM inhibitor with an IC50of 6.2 nM for ATM enzyme, and an IC of 0.3150M for ATM in cell.Purity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.62%Clinical Data: No Development

36、ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AZD0156.html AZD0156 HYPERLINK https:/www.MedChemE/AZD0156.html HYPERLINK https:/www.MedChemE/AZD1390.html AZD1390Cat. No.: HY-100016 Cat. No.: HY-109566AZD0156 is a potent, selective and orally activeATM inhibitor wi

37、th an IC of 0.58 nM. AZD015650inhibits the ATM-mediated signaling, preventsDNA damage checkpoint activation, disrupts DNAdamage repair, and induces tumor cell apoptosis.AZD1390 is a potent, highly selective, orallybioavailable, brain-penetrant ATM inhibitorwith an IC of 0.78 nM in cell.50Purity: 99.

38、82%Clinical Data: Phase 1Size: 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.97%Clinical Data: Phase 1Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/AZD6738.html Ceralasertib HYPERLINK https:/www.MedChemE/AZD6738.html HYPERLINK https:/www.MedChemE/cgk733.html CGK733(AZD6738)

39、Cat. No.: HY-19323Cat. No.: HY-15520Ceralasertib (AZD6738) is an orally active andbioavailable inhibitor of ATR kinase with an ICof 1 nM.50CGK733 is a potent ATM/ATR inhibitor, used forthe research of cancer.Purity: 99.76%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.8

40、3%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/CP-466722.html CP-466722 HYPERLINK https:/www.MedChemE/CP-466722.html HYPERLINK https:/www.MedChemE/BAY-1895344.html ElimusertibCat. No.: HY-11002(BAY 1895344) Cat. No.: HY-101566CP-4

41、66722 is a rapidly reversible inhibitor ofATM, with an IC of 4.1 M, and has no effects50on PI3K or closely related PI3K-like proteinkinase (PIKK) family members.Elimusertib (BAY-1895344) is a potent, orallyactive and selective ATR inhibitor with an IC50of 7 nM. Elimusertib has anti-tumor activity.El

42、imusertib can be used for the research of solidtumors and lymphomas.Purity: 99.40%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.99%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: sale

43、sMedChemE HYPERLINK https:/www.MedChemE/BAY-1895344_hydrochloride.html Elimusertib HYPERLINK https:/www.MedChemE/BAY-1895344_hydrochloride.html HYPERLINK https:/www.MedChemE/BAY-1895344_hydrochloride.html hydrochloride(BAY 1895344 hydrochloride) Cat. No.: HY-101566A HYPERLINK https:/www.MedChemE/etp

44、-46464.html ETP-46464Cat. No.: HY-15521Elimusertib (BAY 1895344) hydrochloride is apotent, orally active and selective ATR inhibitorwith an IC of 7 nM. Elimusertib hydrochloride50has anti-tumor activity. Elimusertib hydrochloridecan be used for the research of solid tumors andlymphomas.ETP-46464 is

45、an effective mTOR and ATRinhibitor with IC s of 0.6 and 14 nM,50respectively.Purity: 99.84%Clinical Data: Phase 2Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.01%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/garcinone-c.html Garcinone HYPERLINK https:/www.MedChemE/garcinone-c.html HYPERLINK https:/www.MedChemE/garcinone-c.html CCat. No.: HY-N6954 HYPERLINK https:/www.MedChemE/atr-inhibitor-2.html Gartisertib(VX-803; M4344; ATR inhibitor 2) Cat. No.: HY-136270Garcinone C, a xanthone deriv