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Chemical Structure| 172889-27-9 Chemical Structure| 172889-27-9

Structure of PP2
CAS No.: 172889-27-9

Chemical Structure| 172889-27-9

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PP2 is a reversible, ATP-competitive inhibitor of Src family kinases with IC50 values of 4 nM for Lck and 5 nM for Fyn.

Synonyms: PP2

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Product Details of PP2

CAS No. :172889-27-9
Formula : C15H16ClN5
M.W : 301.77
SMILES Code : CC(C)(C)N1N=C(C2=C1N=CN=C2N)C1=CC=C(Cl)C=C1
Synonyms :
PP2
MDL No. :MFCD01568210
InChI Key :PBBRWFOVCUAONR-UHFFFAOYSA-N
Pubchem ID :4878

Safety of PP2

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PP2

RTK

Isoform Comparison

Biological Activity

Target
  • Fyn

    Fyn, IC50:5 nM

  • Lck

    LCK, IC50:4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
NB4 cells 10 μM 48 h PP2 accelerated ATRA-induced G1/0 arrest and differentiation marker expression. PMC3310950
HL-60 cells 10 μM 48 h PP2 accelerated ATRA-induced G1/0 arrest and differentiation marker expression. PMC3310950
Vascular smooth muscle cells (VSMC) 10 μM 5 min PP2 inhibited Ang II-induced c-Src phosphorylation, indicating the role of PP2 in inhibiting c-Src activation. PMC8953456
Rat mesenteric arteries 10 μM 15 min To investigate the effect of PP2 on SPC-induced potentiation of vasoconstriction. The results showed that PP2 strongly suppressed SPC-induced potentiation of depolarization-induced contraction PMC4362402
SW620 human colon cancer cells 10 μM PP2 inhibited the phosphorylation of c-Src, while PP3 had no such effect. PMC5648044
COS-7 cells 10 µM 2 h PP2 inhibited Netrin-1-induced Rac1 activation, indicating the role of Src family kinases in Netrin-1 signaling. PMC2172574
N1E-115 mouse neuroblastoma cells 10 µM 2 h PP2 inhibited Netrin-1-induced tyrosine phosphorylation of DCC, indicating the role of Src family kinases in DCC phosphorylation. PMC2172574

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice NOX5 transgenic mice Not specified 10 µmol/L Not specified PP2 reduced the vascular contractile responses in NOX5 transgenic mice, indicating the role of PP2 in inhibiting c-Src-mediated vascular contraction. PMC8953456
C57BL/6 mice Μ+/- mice Intraperitoneal injection 5 mg/Kg Once daily for 5 days PP2 attenuated morphine tolerance, while PP3 had no such effect. PMC5648044
Rat Embryonic spinal commissural neurons In vitro culture 10 µM 2 hours pretreatment, 10 minutes Netrin-1 stimulation PP2 inhibited Netrin-1-induced tyrosine phosphorylation of DCC and axon outgrowth, indicating the critical role of Src family kinases in Netrin-1 signaling. PMC2172574

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01434472 Post-Transplant Lymphoprolifer... More >>ative Disorder Recurrent Adult Diffuse Large Cell Lymphoma Recurrent B-Cell Non-Hodgkin Lymphoma Recurrent Burkitt Lymphoma Refractory B-Cell Non-Hodgkin Lymphoma Refractory Burkitt Lymphoma Refractory Diffuse Large B-Cell Lymphoma Less << Phase 2 Recruiting September 24, 2022 United States, Washington ... More >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Ajay K. Gopal    206-288-2037    agopal@u.washington.edu    Principal Investigator: Ajay K. Gopal Less <<
NCT00438880 Adult Non-Hodgkin Lymphoma ... More >> Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue Nodal Marginal Zone Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Small Lymphocytic Lymphoma Splenic Marginal Zone Lymphoma Waldenstrom Macroglobulinemia Less << Phase 1 Phase 2 Completed - United States, Iowa ... More >> University of Iowa/Holden Comprehensive Cancer Center Iowa City, Iowa, United States, 52242 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 Less <<
NCT00119392 B-cell Chronic Lymphocytic Leu... More >>kemia Nodal Marginal Zone B-cell Lymphoma Recurrent Adult Burkitt Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Adult Diffuse Mixed Cell Lymphoma Recurrent Adult Diffuse Small Cleaved Cell Lymphoma Recurrent Adult Grade III Lymphomatoid Granulomatosis Recurrent Adult Immunoblastic Large Cell Lymphoma Recurrent Adult Lymphoblastic Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Small Lymphocytic Lymphoma Splenic Marginal Zone Lymphoma Waldenstr?m Macroglobulinemia Less << Phase 2 Completed - United States, Washington ... More >> Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium Seattle, Washington, United States, 98109 Less <<
NCT00577278 Graft Versus Host Disease ... More >> Leukemia Lymphoma Less << Phase 2 Active, not recruiting March 2019 United States, California ... More >> City of Hope Medical Center Duarte, California, United States, 91010-3000 Less <<
NCT00119392 - Completed - -
NCT00695409 - Completed - -
NCT02366663 Recurrent Diffuse Large B-Cell... More >> Lymphoma Refractory Diffuse Large B-Cell Lymphoma Less << Phase 3 Terminated(Withdrawal of spons... More >>or support) Less << - United States, California ... More >> City of Hope Medical Center Duarte, California, United States, 91010 United States, New York Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 Less <<
NCT00438880 - Completed - -
NCT02366663 - Terminated(Withdrawal of spons... More >>or support) Less << - -
NCT00797797 Fibromyalgia Phase 3 Completed - -
NCT02320292 Stage I Grade 1 Follicular Lym... More >>phoma Stage I Grade 2 Follicular Lymphoma Stage II Grade 1 Contiguous Follicular Lymphoma Stage II Grade 1 Non-Contiguous Follicular Lymphoma Stage II Grade 2 Contiguous Follicular Lymphoma Stage II Grade 2 Non-Contiguous Follicular Lymphoma Stage III Grade 1 Follicular Lymphoma Stage III Grade 2 Follicular Lymphoma Stage IV Grade 1 Follicular Lymphoma Stage IV Grade 2 Follicular Lymphoma Less << Phase 3 Recruiting January 2026 United States, Iowa ... More >> University of Iowa/Holden Comprehensive Cancer Center Recruiting Iowa City, Iowa, United States, 52242 Contact: George J. Weiner    800-237-1225    george-weiner@uiowa.edu    Principal Investigator: George J. Weiner          United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Clinical Trials Referral Office    855-776-0015       Principal Investigator: Thomas E. Witzig Less <<
NCT00797797 - Completed - -
NCT00038623 Lymphoma, Mantle-Cell Phase 2 Completed - United States, Texas ... More >> MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT00695409 Lymphoma Phase 2 Completed - United States, California ... More >> City of Hope Medical Center Duarte, California, United States, 91010-3000 Less <<
NCT01686165 Anaplastic Large Cell Lymphoma... More >> Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Mantle Cell Lymphoma Less << Phase 2 Completed - United States, Arizona ... More >> University of Arizona Cancer Center Tucson, Arizona, United States, 85724-5024 Less <<
NCT02315287 Type 2 Diabetes Phase 4 Recruiting December 2018 Korea, Republic of ... More >> Seoul National University Bundang Hospital Recruiting Seongnam, Gyeonggi, Korea, Republic of, 463-707 Contact: Soo Lim, MD, PHD    82-31-787-7035    limsoo@snu.ac.kr    Contact: Eu Jeong Ku, MD    82-31-787-6232    eujeong.ku@gmail.com    Principal Investigator: Soo Lim, MD, PHD Less <<
NCT01686165 - Completed - -
NCT02338921 Type 2 Diabetes Phase 4 Recruiting December 2018 Korea, Republic of ... More >> Soo Lim Recruiting Seongnam, Gyeonggi, Korea, Republic of, 463-707 Contact: Dong Hwa Lee, MD Less <<
NCT00591630 Diffuse Large Cell Lymphoma ... More >> Lymphoma Less << Phase 2 Active, not recruiting November 2019 United States, Texas ... More >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT01973062 Primary Central Nervous System... More >> Non-Hodgkin Lymphoma Less << Phase 2 Terminated(Funding Unavailable... More >>) Less << - United States, Ohio ... More >> Cleveland Clinic Taussig Cancer Institute, Case Comprehensive Cancer Center Cleveland, Ohio, United States, 44195 Less <<
NCT01973062 - Terminated(Funding Unavailable... More >>) Less << - -
NCT03233672 Prostate Cancer Not Applicable Completed - -
NCT00493467 Lymphoma Phase 2 Completed - United States, Texas ... More >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT02036554 Kidney; Complications, Allogra... More >>ft Less << Phase 4 Unknown December 2015 Korea, Republic of ... More >> division of nephrology;Seoul St Mary's Hospital Recruiting Seoul, Korea, Republic of Contact: Chul Woo Yang    82-2-2258-6851    yangch@catholic.ac.kr Less <<
NCT00387023 Non-Hodgkin's Lymphoma ... More >> Lymphoma Less << Not Applicable Completed - United States, Texas ... More >> UT MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT00064246 Post-transplant Lymphoprolifer... More >>ative Disorder Recurrent Adult Burkitt Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Stage III Adult Burkitt Lymphoma Stage III Adult Diffuse Large Cell Lymphoma Stage IV Adult Burkitt Lymphoma Stage IV Adult Diffuse Large Cell Lymphoma Waldenstr?m Macroglobulinemia Less << Phase 1 Phase 2 Completed - United States, Maryland ... More >> AIDS - Associated Malignancies Clinical Trials Consortium Rockville, Maryland, United States, 20850 Less <<
NCT00477815 Multiple Myeloma and Plasma Ce... More >>ll Neoplasm Less << Phase 1 Completed - United States, Minnesota ... More >> Mayo Clinic Rochester, Minnesota, United States, 55905 Less <<
NCT00036855 AIDS-related Peripheral/System... More >>ic Lymphoma AIDS-related Primary CNS Lymphoma Post-transplant Lymphoproliferative Disorder Recurrent Childhood Large Cell Lymphoma Recurrent Childhood Lymphoblastic Lymphoma Recurrent Childhood Small Noncleaved Cell Lymphoma Recurrent/Refractory Childhood Hodgkin Lymphoma Less << Phase 1 Terminated(Administratively co... More >>mplete.) Less << - United States, California ... More >> Children's Oncology Group Arcadia, California, United States, 91006-3776 Less <<
NCT00290511 Lymphoma Phase 2 Active, not recruiting August 24, 2019 United States, Texas ... More >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT00387023 - Completed - -
NCT03077360 Diabetes Mellitus, Type 2 ... More >> Pre-diabetes Obesity Less << Not Applicable Recruiting January 31, 2021 United States, Colorado ... More >> University of Colorado Recruiting Aurora, Colorado, United States, 80045 Contact: Simona Zarini, PhD    303-724-3968    Simona.Zarini@ucdenver.edu Less <<
NCT02185339 Laparoscopic Renal Surgery ... More >> Laparoscopy Muscle Relaxation Less << Phase 4 Completed - Korea, Republic of ... More >> Seoul St. Mary's Hospital Seoul, Korea, Republic of, 137-701 Less <<
NCT00031642 Lymphoma Phase 1 Phase 2 Completed - United States, Nebraska ... More >> UNMC Eppley Cancer Center at the University of Nebraska Medical Center Omaha, Nebraska, United States, 68198-7680 Less <<
NCT02407626 Myocardial Ischemia Not Applicable Terminated(Very low patient re... More >>cruitment, changed insurance requirements) Less << - Switzerland ... More >> Triemli City Hospital Zurich, Switzerland, 8063 Less <<
NCT00058292 Lymphoma Phase 1 Completed - United States, Illinois ... More >> Hematology-Oncology Associates of Illinois Chicago, Illinois, United States, 60611-2998 Robert H. Lurie Comprehensive Cancer Center at Northwestern University Chicago, Illinois, United States, 60611-3013 United States, Minnesota Mayo Clinic Cancer Center Rochester, Minnesota, United States, 55905 Less <<
NCT01041144 Type 2 Diabetes ... More >> Lifestyle Intervention Glucose Control Internet Communication Less << Not Applicable Completed - Korea, Republic of ... More >> Seoul St. Mary's Hospital Seoul, Korea, Republic of, 137-041 Less <<
NCT00017381 Contiguous Stage II Adult Diff... More >>use Large Cell Lymphoma Contiguous Stage II Adult Diffuse Small Cleaved Cell Lymphoma Contiguous Stage II Grade 1 Follicular Lymphoma Contiguous Stage II Grade 2 Follicular Lymphoma Contiguous Stage II Grade 3 Follicular Lymphoma Contiguous Stage II Mantle Cell Lymphoma Contiguous Stage II Marginal Zone Lymphoma Contiguous Stage II Small Lymphocytic Lymphoma Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue Noncontiguous Stage II Adult Diffuse Large Cell Lymphoma Noncontiguous Stage II Adult Diffuse Small Cleaved Cell Lymphoma Noncontiguous Stage II Grade 1 Follicular Lymphoma Noncontiguous Stage II Grade 2 Follicular Lymphoma Noncontiguous Stage II Grade 3 Follicular Lymphoma Noncontiguous Stage II Mantle Cell Lymphoma Noncontiguous Stage II Marginal Zone Lymphoma Noncontiguous Stage II Small Lymphocytic Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Adult Diffuse Small Cleaved Cell Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Small Lymphocytic Lymphoma Stage I Adult Diffuse Large Cell Lymphoma Stage I Adult Diffuse Small Cleaved Cell Lymphoma Stage I Grade 1 Follicular Lymphoma Stage I Grade 2 Follicular Lymphoma Stage I Grade 3 Follicular Lymphoma Stage I Mantle Cell Lymphoma Stage I Marginal Zone Lymphoma Stage I Small Lymphocytic Lymphoma Stage III Adult Diffuse Large Cell Lymphoma Stage III Adult Diffuse Small Cleaved Cell Lymphoma Stage III Grade 1 Follicular Lymphoma Stage III Grade 2 Follicular Lymphoma Stage III Grade 3 Follicular Lymphoma Stage III Mantle Cell Lymphoma Stage III Marginal Zone Lymphoma Stage III Small Lymphocytic Lymphoma Stage IV Adult Diffuse Large Cell Lymphoma Stage IV Adult Diffuse Small Cleaved Cell Lymphoma Stage IV Grade 1 Follicular Lymphoma Stage IV Grade 2 Follicular Lymphoma Stage IV Grade 3 Follicular Lymphoma Stage IV Mantle Cell Lymphoma Stage IV Marginal Zone Lymphoma Stage IV Small Lymphocytic Lymphoma Waldenstr?m Macroglobulinemia Less << Early Phase 1 Completed - United States, Maryland ... More >> Johns Hopkins University Baltimore, Maryland, United States, 21287-8936 Less <<
NCT00437554 Diabetes Mellitus, Type 2 Phase 3 Completed - Korea, Republic of ... More >> Handok Seoul, Korea, Republic of Less <<
NCT00012298 Extranodal Marginal Zone B-cel... More >>l Lymphoma of Mucosa-associated Lymphoid Tissue Nodal Marginal Zone B-cell Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Small Lymphocytic Lymphoma Splenic Marginal Zone Lymphoma Waldenstr?m Macroglobulinemia Less << Phase 1 Phase 2 Terminated(Trial completed pre... More >>maturely.) Less << - United States, Minnesota ... More >> Mayo Clinic Rochester, Minnesota, United States, 55905 Less <<
NCT02185339 - Completed - -
NCT00807365 - Terminated(PI left JHU) - -
NCT00807365 Elderly Phase 2 Terminated(PI left JHU) - United States, Maryland ... More >> Johns Hopkins Bayview Medical Center Baltimore, Maryland, United States, 21224 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Less <<
NCT00012298 - Terminated(Trial completed pre... More >>maturely.) Less << - -
NCT01047605 Healthy Phase 1 Completed - Germany ... More >> Neurocode AG Wetzlar, Germany, D-35578 Less <<
NCT00005592 Lymphoma Phase 2 Completed - United States, Alabama ... More >> University of Alabama at Birmingham Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3300 United States, District of Columbia Lombardi Cancer Center Washington, District of Columbia, United States, 20007 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.57mL

3.31mL

1.66mL

33.14mL

6.63mL

3.31mL

References

 

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