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1、 HYPERLINK https:/www.MedChemE/Targets/Btk.html BtkBruton tyrosine kinaseBruton tyrosine kinase (Btk) is a member of the Tec family kinases with a well-characterized role in B-cell antigen receptor(BCR)-signaling and B-cell activation.Btk plays a crucial role in B cell development and activation thr

2、ough the BCR signaling pathway and represents a new target fordiseases characterized by inappropriate B cell activity. Btk is a kinase expressed exclusively in B cells and myeloid cells and has awell characterized, vital role in B cells highlighted by the human primary immune deficiency disease, X-l

3、inked agammaglobulinemia(XLA), which results from mutation in the Btk gene. Btk plays an essential role in the BCR signaling pathway. Antigen binding to theBCR results in B cell receptor oligomerization, Syk and Lyn kinase activation, followed by Btk kinase activation. Once activated, Btkforms a sig

4、naling complex with proteins such as BLNK, Lyn, and Syk and phosphorylates phospholipase C (PLC)2. This leads todownstream release of intracellular Ca2+ stores and propagation of the BCR signaling pathway through extracellularsignal-regulated kinase and NF-B signaling, ultimately resulting in transc

5、riptional changes to foster B cell survival, proliferation,and/or differentiation.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Btk.html Btk HYPERLINK https:/www.MedChemE/Targets/Btk.html HYPERLINK https:/www.MedChemE/Targets/Btk.html Inhibitors HYPERLINK https:/www.MedChemE/btk-inhibitor-1.h

6、tml (Rac)-IBT6A HYPERLINK https:/www.MedChemE/btk-inhibitor-1.html HYPERLINK https:/www.MedChemE/btk-inhibitor-1-hydrochloride.html (Rac)-IBT6A HYPERLINK https:/www.MedChemE/btk-inhibitor-1-hydrochloride.html HYPERLINK https:/www.MedChemE/btk-inhibitor-1-hydrochloride.html hydrochlorideCat. No.: HY-

7、13036 Cat. No.: HY-13036C(Rac)-IBT6A is a racemate of IBT6A. IBT6A is animpurity of Ibrutinib. IBT6A can be used insynthesis of IBT6A Ibrutinib dimer and IBT6Aadduct. Ibrutinib is a selective, irreversible Btkinhibitor with an IC of 0.5 nM.50(Rac)-IBT6A hydrochloride is a racemate of IBT6Ahydrochlor

8、ide. IBT6A is an impurity of Ibrutinib.IBT6A can be used in synthesis of IBT6A Ibrutinibdimer and IBT6A adduct. Ibrutinib is a selective,irreversible Btk inhibitor with an IC of 0.5 nM.50Purity: 98.18%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinic

9、al Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/s-sunvozertinib.html (S)-Sunvozertinib(S)-DZD9008) Cat. No.: HY-132842A HYPERLINK https:/www.MedChemE/BGB-3111.html ()-Zanubrutinib()-BGB-3111) Cat. No.: HY-101474(S)-Sunvozertinib (S)-DZD9008), the S-enantiomerof Sunvoze

10、rtinib, shows inhibitory activityagainst EGFR exon 20 NPH and ASV insertions, EGFRL858R/T790M mutation and Her2 exon20 YVMAinsertion (IC =51.2 nM, 51.9 nM, 1 nM, and 21.250nM, respectively).()-Zanubrutinib ()-BGB-3111) is a potent,selective and orally available Brutons tyrosinekinase (Btk) inhibitor

11、.Purity: 99.14%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.73%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Acalabrutinib.html Acalabrutinib(ACP-196) Cat. No.: HY-17600 HYPERLINK https:/www.MedChem

12、E/acalabrutinib-d4.html Acalabrutinib-d4(ACP-196-d4) Cat. No.: HY-17600SAcalabrutinib (ACP-196) is an orally active,irreversible, and highly selectivesecond-generation BTK inhibitor. Acalabrutinibbinds covalently to Cys481 in the ATP-bindingpocket of BTK.Acalabrutinib D4 (ACP-196 D4) is a deuteriuml

13、abeled Acalabrutinib. Acalabrutinib (ACP-196) isan orally active, irreversible, and highlyselective second-generation BTK inhibitor.Purity: 99.94%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/

14、www.MedChemE/acp-5862.html ACP-5862 HYPERLINK https:/www.MedChemE/acp-5862.html HYPERLINK https:/www.MedChemE/acp-5862-d4.html ACP-5862-d4Cat. No.: HY-135334 Cat. No.: HY-135334SACP-5862 is a major active, circulating,pyrrolidine ring-opened metabolite ofAcalabrutinib with an IC50 of 5.0 nM for Brut

15、ontyrosine kinase (BTK). ACP5862 is a weaktimedependent inactivator of CYP3A4 and CYP2C8.ACP-5862-d4 is deuterium labeled ACP-5862.ACP-5862 is a major active, circulating,pyrrolidine ring-opened metabolite ofAcalabrutinib with an IC50 of 5.0 nM for Brutontyrosine kinase (BTK).Purity: 98.09%Clinical

16、Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data:Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ARQ_531.html ARQ HYPERLINK https:/www.MedChemE/ARQ_531.html HYPERLINK https:/www.MedChemE/ARQ_531.html 531 HYPERLINK https:/www.MedChemE/ARQ_531.html HYPERLINK https:/ww

17、w.MedChemE/as-1763.html AS-1763(MK-1026) Cat. No.: HY-112215Cat. No.: HY-132877ARQ 531 (MK-1026) is a reversible non-covalent andorally active inhibitor of Brutons TyrosineKinase (BTK), with IC s of 0.85 nM and 0.39 nM50for WT-BTK and C481S-BTK, respectively.AS-1763 is a potent, selective, noncovale

18、nt, andorally available inhibitor of Brutons tyrosinekinase (IC = 0.85 nM).50Purity: 99.24%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChe

19、mE HYPERLINK https:/www.MedChemE/atuzabrutinib.html Atuzabrutinib(SAR 444727; PRN473) Cat. No.: HY-132808 HYPERLINK https:/www.MedChemE/avitinib.html Avitinib(Abivertinib; AC0010) Cat. No.: HY-19816Atuzabrutinib (SAR 444727) is a potent, selectivereversible inhibitor of Btk (Brutons tyrosinekinase)

20、inhibitor. Atuzabrutinib inhibitsneutrophil recruitment via inhibition ofmacrophage antigen-1 signalling.Avitinib (AC0010) is an irreversible,mutant-selective EGFR inhibitor that effectivelyinhibits EGFR T790M resistance mutations innon-small cell lung cancer (NSCLC). Abivertinib isalso a novel BTK

21、inhibitor.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/bcpyr.html BCPyr HYPERLINK https:/www.MedChemE/bcpyr.html HYPERLINK https:/www.MedChemE/biib068.html BIIB068Cat. No.: HY-142621 C

22、at. No.: HY-131342BCPyr is a new candidate BTK degrader (DC =50800 nM).BIIB068 is a potent, selective, reversible andorally active BTK inhibitor with an IC of 1 nM50and a K of 0.3 nM. BIIB068 shows mored400-fold selective for BTK than otherkinases. BIIB068 has the potential for autoimmunediseases re

23、search.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.20%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/biib091.html BIIB091 HYPERLINK https:/www.MedChemE/biib091.html HYPERLINK https:/www.MedChemE/

24、blk-in-1.html BLK-IN-1Cat. No.: HY-139984 Cat. No.: HY-144283BIIB091 is a highly selective, reversible BTKinhibitor for treating autoimmune diseases.BLK-IN-1 (compound 1) is a selective and covalentinhibitor of B-Lymphoid tyrosine kinase (BLK)and BTK, with IC s of 18.8 nM and 20.5 nM,50respectively.

25、 BLK-IN-1 can be used for theresearch of cancer.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/blk-in-2.html BLK-IN-2 HYPERLINK https:/www.MedChemE/blk-in-2.html H

26、YPERLINK https:/www.MedChemE/BMS-935177.html BMS-935177Cat. No.: HY-144288 Cat. No.: HY-101793BLK-IN-2 (compound 25) is a potent and selectiveirreversible inhibitor of B-Lymphoid tyrosinekinase (BLK), with an IC of 5.9 nM. BLK-IN-250also inhibits BTK (IC =202.0 nM). BLK-IN-2 shows50potent antiprolif

27、erative activities againstseveral lymphoma cells.BMS-935177 is a potent and selective reversibleinhibitor of Brutons tyrosine kinase (Btk) withan IC of 3 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.33%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg,

28、5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/BMS-986142.html BMS-986142 HYPERLINK https:/www.MedChemE/BMS-986142.html HYPERLINK https:/www.MedChemE/bms-986143.html BMS-986143Cat. No.: HY-101856 Cat. No.: HY-145373BMS-986142 is a potent and highly selectivereversible inhibitor of B

29、rutons tyrosine kinase(BTK) with an IC of 0.5 nM.50BMS-986143 is an orally active, reversible BTKinhibitor with an IC of 0.26 nM. BMS-986143 also50inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK withIC s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 2150nM, respectively. BMS-986143 can be used for theresearch

30、 of autoimmune diseases.Purity: 99.53%Clinical Data: LaunchedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/BMX-IN-1.html BMX-IN-1(BMX kinase inhibitor) Cat. No.: HY-80002 HYPERLINK https:/www.MedCh

31、emE/BMS-986195.html Branebrutinib(BMS-986195) Cat. No.: HY-112161BMX-IN-1 is a selective, irreversible inhibitor ofbone marrow tyrosine kinase on chromosome X(BMX) that targets Cys496 in the BMX ATPbinding domain with an IC of 8 nM, also targets50the related Brutons tyrosine kinase (BTK) withan IC v

32、alue of 10.4 nM, but is more50Purity: 99.04%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mgBranebrutinib (BMS-986195) is a highly potent,selective covalent, irreversible inhibitor ofBrutons tyrosine kinase (BTK), with an IC of500.1 nM.Purity: 99.56%Clinical Data: No

33、Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/SNS-062.html BTK HYPERLINK https:/www.MedChemE/SNS-062.html HYPERLINK https:/www.MedChemE/SNS-062.html IN-1(SNS062 analog) Cat. No.: HY-101941 HYPERLINK https:/www.MedChemE/btk-inhibitor-10.html BT

34、K HYPERLINK https:/www.MedChemE/btk-inhibitor-10.html HYPERLINK https:/www.MedChemE/btk-inhibitor-10.html inhibitor HYPERLINK https:/www.MedChemE/btk-inhibitor-10.html HYPERLINK https:/www.MedChemE/btk-inhibitor-10.html 10Cat. No.: HY-125997BTK IN-1 (SNS062 analog) is a potent BTKinhibitor, with an

35、IC of 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/btk-inhibitor-13.html BTK HYPERLINK https:/www.MedChemE/btk-inhibitor-13.html HYPERLINK https:/www.MedChemE/btk-inhibitor-13.html inhibitor HYPERLINK https:/www.MedChemE/btk-inhibitor-13.html HYPERLINK http

36、s:/www.MedChemE/btk-inhibitor-13.html 13 HYPERLINK https:/www.MedChemE/btk-inhibitor-13.html HYPERLINK https:/www.MedChemE/btk-inhibitor-17.html BTK HYPERLINK https:/www.MedChemE/btk-inhibitor-17.html HYPERLINK https:/www.MedChemE/btk-inhibitor-17.html inhibitor HYPERLINK https:/www.MedChemE/btk-inh

37、ibitor-17.html HYPERLINK https:/www.MedChemE/btk-inhibitor-17.html 17Cat. No.: HY-130255 Cat. No.: HY-131705BTK inhibitor 13 (compound 8) is a potent andselective Brutons tyrosine kinase (BTK)inhibitor with an IC of 1.2 nM.50BTK inhibitor 17 is a potent and orally activeirreversible BTK inhibitor wi

38、th an IC of 2.150nM. BTK inhibitor 17 can be used for rheumatoidarthritis research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.98%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/btk-inhibitor-18.h

39、tml BTK HYPERLINK https:/www.MedChemE/btk-inhibitor-18.html HYPERLINK https:/www.MedChemE/btk-inhibitor-18.html inhibitor HYPERLINK https:/www.MedChemE/btk-inhibitor-18.html HYPERLINK https:/www.MedChemE/btk-inhibitor-18.html 18 HYPERLINK https:/www.MedChemE/btk-inhibitor-18.html HYPERLINK https:/ww

40、w.MedChemE/btk-inhibitor-19.html BTK HYPERLINK https:/www.MedChemE/btk-inhibitor-19.html HYPERLINK https:/www.MedChemE/btk-inhibitor-19.html inhibitor HYPERLINK https:/www.MedChemE/btk-inhibitor-19.html HYPERLINK https:/www.MedChemE/btk-inhibitor-19.html 19Cat. No.: HY-132196 Cat. No.: HY-139881BTK

41、inhibitor 18 is a potent, selective,orallyactive and covalent Btk inhibitor with a IC of50142 nM. BTK inhibitor 18 has anti-inflammatoryactivities.BTK inhibitor 19 is a highly selective, covalentBTK inhibitor (IC = 2.7 nM).50Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg,

42、50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Btk_inhibitor_2.html Btk HYPERLINK https:/www.MedChemE/Btk_inhibitor_2.html HYPERLINK https:/www.MedChemE/Btk_inhibitor_2.html inhibitor HYPERLINK https:/www.MedChemE/Btk_inhibitor_2.html HYP

43、ERLINK https:/www.MedChemE/Btk_inhibitor_2.html 2 HYPERLINK https:/www.MedChemE/Btk_inhibitor_2.html HYPERLINK https:/www.MedChemE/btk-inhibitor-20.html BTK HYPERLINK https:/www.MedChemE/btk-inhibitor-20.html HYPERLINK https:/www.MedChemE/btk-inhibitor-20.html inhibitor HYPERLINK https:/www.MedChemE

44、/btk-inhibitor-20.html HYPERLINK https:/www.MedChemE/btk-inhibitor-20.html 20(BGB-3111 analog) Cat. No.: HY-101766Cat. No.: HY-143730Btk inhibitor 2 (BGB-3111 analog) is a Brutonstyrosine kinase (BTK) inhibitor extracted frompatent US 20170224688 A1.BTK inhibitor 20 is a potent BTK inhibitor withan

45、IC of 8 nM.50Purity: 99.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/btk-in-5.html BTK-IN-5 HYPERLI

46、NK https:/www.MedChemE/btk-in-5.html HYPERLINK https:/www.MedChemE/btk-in-6.html BTK-IN-6Cat. No.: HY-115876 Cat. No.: HY-142932BTK-IN-5 is a covalent BTK inhibitor for treatingmedical conditions such as cardiovasculardiseases, respiratory diseases, inflammation, anddiabetes.BTK-IN-6 is a potent inh

47、ibitor of BrutonsTyrosine Kinase (BTK). BTK is a member of the Tecfamily of tyrosine kinases and plays an importantrole in the regulation of early B-cell developmentand mature B-cell activation and survival.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No

48、 Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/btk-in-7.html BTK-IN-7 HYPERLINK https:/www.MedChemE/btk-in-7.html HYPERLINK https:/www.MedChemE/btk-in-8.html BTK-IN-8Cat. No.: HY-143900 Cat. No.: HY-145884BTK-IN-7 is a potent and selective inhibitor ofBTK (IC =4.0 nM). BTK-IN-7

49、has high selectivity50in both enzymatic (ITK 250-fold, EGFR2500-fold) and cellular levels(ITK227-fold, EGFR 27-fold). BTK-IN-7 also haspotent antitumor activity.BTK-IN-8 is a potent selective peripheral covalentBTK inhibitor (IC =0.22 nM; =0.91 nM).50 KdBTK-IN-8 has good whole blood CD69 cellularpot

50、ency (IC =0.029 M).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/btk-in-9.html BTK-IN-9 HYPERLINK https:/www.MedChemE/btk-in-9.html HYPERLINK https:/www.MedChemE/CGI-1746.html CGI-174

51、6Cat. No.: HY-115944 Cat. No.: HY-11999BTK-IN-9 is a reversible BTK inhibitors withpotent antiproliferative activity in mantle celllymphoma. BTK-IN-9 specifically disturbsmitochondrial membrane potential and increasesreactive oxygen species level in Z138 cells.CGI-1746 is a potent and highly selecti

52、veinhibitor ofthe Btk with IC of 1.950nM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.01%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/chmfl-btk-01.html CHMFL-BTK-01 HYPERLINK https:/www.MedChemE/chmfl-

53、btk-01.html HYPERLINK https:/www.MedChemE/chmfl-egfr-202.html CHMFL-EGFR-202Cat. No.: HY-101521 Cat. No.: HY-101522CHMFL-BTK-01 (compound 9) is a highly selectiveirreversible BTK inhibitor, with an IC of 7 nM.50CHMFL-BTK-01 (compound 9) potently inhibited BTKY223 auto-phosphorylation.CHMFL-EGFR-202

54、is a potent, irreversible inhibitorof epidermal growth factor receptor (EGFR)mutant kinase, with IC s of 5.3 nM and 8.3 nM for50drug-resistant mutant EGFR T790M and WT EGFRkinases, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development

55、ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cnx-500.html CNX-500 HYPERLINK https:/www.MedChemE/cnx-500.html HYPERLINK https:/www.MedChemE/CNX-774.html CNX-774Cat. No.: HY-100338 Cat. No.: HY-13943CNX-500 is a probe consisting of a covalent Btkinhibitor (CC-292) chemically linked to biotin

56、.CNX-500 retains inhibitory activity against Btk(IC of 0.5 nM) and the ability to form a50covalent bond with Btk.CNX-774 is an orally active, irreversible andselective BTK inhibitor, with an IC of 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.91%Clinical Data: No Development Re

57、portedSize: 5 mg HYPERLINK https:/www.MedChemE/edralbrutinib.html Edralbrutinib(TG-1701) Cat. No.: HY-137438 HYPERLINK https:/www.MedChemE/egfr-in-40.html EGFR-IN-40Cat. No.: HY-143901Edralbrutinib (TG-1701) is a potent BTKinhibitor.EGFR-IN-40 (compound 3z) is a potent BTK, EGFR,and ITK inhibitor wi

58、th IC values of 1.2 nM, 5.350nM, and 46.1 nM, respectively.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/elsubrutinib.html Elsubrutinib(ABBV-105) Cat. No.: HY-109143 HYPERLINK https:/ww

59、w.MedChemE/GDC-0853.html Fenebrutinib(GDC-0853) Cat. No.: HY-19834Elsubrutinib (ABBV-105) is an orally active,potent, selective and irreversible Brutonstyrosine kinase (BTK) inhibitorThe IC of50Elsubrutinib for BTK catalytic domain is 0.18 M.Elsubrutinib can be used for the research ofinflammatory d

60、isease.Fenebrutinib (GDC-0853) is a potent, selective,orally available, and noncovalent brutonstyrosine kinase (Btk) inhibitor with Ks of 0.91inM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and theC481S, C481R, T474I, T474M mutants.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 m

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