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Chemical Structure| 803712-67-6 Chemical Structure| 803712-67-6

Structure of Obatoclax
CAS No.: 803712-67-6

Chemical Structure| 803712-67-6

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Obatoclax, a Bcl-2 homology domain-3 mimetic, antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 μMol/L), including Mcl-1 (IC50, 2.9 μMol/L) and Bfl-1 (IC50, 5 μMol/L).

Synonyms: GX15-070

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Product Details of Obatoclax

CAS No. :803712-67-6
Formula : C20H19N3O
M.W : 317.38
SMILES Code : COC1=CC(C(N2)=CC3=C2C=CC=C3)=N/C1=C\C4=C(C)C=C(C)N4
Synonyms :
GX15-070
MDL No. :MFCD09833233

Safety of Obatoclax

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

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
H460 NSCLC cells 500 nM 6, 24, 48 hours Obatoclax disrupts BAK/MCL-1 complex PMC3032298
AML ROS-low cells 10µM Inhibited oxidative respiration PMC3595363
5637 cells 28 nM (IC50) 1, 3, 5 days Obatoclax inhibits cell proliferation and clonogenicity, and promotes apoptosis in a dose-dependent manner PMC6470498
TCCSuP cells 70 nM (IC50) 1, 3, 5 days Obatoclax inhibits cell proliferation and clonogenicity, and promotes apoptosis in a dose-dependent manner PMC6470498
T24 cells 20 nM (IC50) 1, 3, 5 days Obatoclax inhibits cell proliferation and clonogenicity, and promotes apoptosis in a dose-dependent manner PMC6470498
TFK-1 0.5 μM 16 hours Obatoclax induced minimal apoptosis alone; however, it increased apoptosis 3- to 13-fold in all three cancer cell lines when combined with Apo2L/TRAIL. PMC2562222
KMBC 0.5 μM 16 hours Obatoclax induced minimal apoptosis alone; however, it increased apoptosis 3- to 13-fold in all three cancer cell lines when combined with Apo2L/TRAIL. PMC2562222
KMCH 0.5 μM 16 hours Obatoclax induced minimal apoptosis alone; however, it increased apoptosis 3- to 13-fold in all three cancer cell lines when combined with Apo2L/TRAIL. PMC2562222
AML CD34+ progenitor cells 250 nM - 10 μM 24 hours Obatoclax induced apoptosis in AML CD34+ progenitor cells with an average IC50 of 3.59 μM. PMC4096127
KTC-1 cells 1 µM to 10 µM 24 hours Obatoclax induced massive apoptosis of KTC-1 cells in a dose-dependent manner, and caused loss of mitochondrial membrane potential, dysfunction of mitochondrial respiration, reduction of cellular glycolysis, autophagy, neutralization of lysosomes, and caspase-related apoptosis. PMC5381260
BCPAP cells 1 µM to 10 µM 24 hours Obatoclax induced massive apoptosis of BCPAP cells in a dose-dependent manner, and caused loss of mitochondrial membrane potential, dysfunction of mitochondrial respiration, reduction of cellular glycolysis, autophagy, neutralization of lysosomes, and caspase-related apoptosis. PMC5381260
K1 cells 1 µM to 10 µM 24 hours Obatoclax induced massive apoptosis of K1 cells in a dose-dependent manner, and caused loss of mitochondrial membrane potential, dysfunction of mitochondrial respiration, reduction of cellular glycolysis, autophagy, neutralization of lysosomes, and caspase-related apoptosis. PMC5381260
Karpas-422 cells 100 nM 24 hours Obatoclax in combination with VSV activated the mitochondrial apoptotic pathway in Karpas-422 cells, leading to caspase-3 and -9 cleavage, cytochrome c release, and BAX translocation. PMC2997588
CD5+ CD19+ CLL cells 100 nM 24 hours Obatoclax in combination with VSV synergistically induced cell death in primary CLL cells, significantly increasing cell mortality. PMC2997588
BxPC-3 0–2.5 μM 24 hours Obatoclax alone or in combination with TRAIL significantly enhanced apoptosis in BxPC-3 cells, as evidenced by increased Annexin V labeling, accompanied by activation of caspase-8, -9, and -3 and cleavage of Bid. PMC2948485
PANC-1 0–2.5 μM 24 hours Obatoclax alone or in combination with TRAIL significantly enhanced apoptosis in PANC-1 cells, as evidenced by increased Annexin V labeling, accompanied by activation of caspase-8, -9, and -3 and cleavage of Bid. PMC2948485
Caco-2 0.33, 1 μM, 3.3 μM 24 hours Evaluate the inhibitory effect of Obatoclax on clinical SARS-CoV-2 isolate infections PMC8843317
Calu-3 0.33, 1 μM, 3.3 μM 24 hours Evaluate the inhibitory effect of Obatoclax on clinical SARS-CoV-2 isolate infections PMC8843317
CHLA05-ATRT 40 nM 24 hours To evaluate the effect of Obatoclax on apoptosis and oxidative stress, results showed that Obatoclax significantly induced oxidative stress and apoptosis. PMC9050713
CHLA02-ATRT 40 nM 24 hours To evaluate the effect of Obatoclax on apoptosis and oxidative stress, results showed that Obatoclax significantly induced oxidative stress and apoptosis. PMC9050713
BT37 40 nM 24 hours To evaluate the effect of Obatoclax on apoptosis and oxidative stress, results showed that Obatoclax significantly induced oxidative stress and apoptosis. PMC9050713
CHLA06-ATRT 40 nM 24 hours To evaluate the effect of Obatoclax on apoptosis and oxidative stress, results showed that Obatoclax significantly induced oxidative stress and apoptosis. PMC9050713
BT-12 40 nM 24 hours To evaluate the effect of Obatoclax on apoptosis and oxidative stress, results showed that Obatoclax significantly induced oxidative stress and apoptosis. PMC9050713
H69 200 nM 24 hours Synergistic growth inhibition of SCLC cells and reduction of MCL-1 expression PMC8285499
H1963 200 nM 24 hours Synergistic growth inhibition of SCLC cells and reduction of MCL-1 expression PMC8285499
H196 200 nM 24 hours Synergistic growth inhibition of SCLC cells and reduction of MCL-1 expression PMC8285499
DMS79 200 nM 24 hours Synergistic growth inhibition of SCLC cells and reduction of MCL-1 expression PMC8285499
H526 200 nM 24 hours Synergistic growth inhibition of SCLC cells and reduction of MCL-1 expression PMC8285499
H82 200 nM 24 hours Synergistic growth inhibition of SCLC cells and reduction of MCL-1 expression PMC8285499
CT26 cells 10 µM or 30 µM 24 hours To evaluate the inhibitory effect of Obatoclax on the migration of CT26 cells. Results showed that Obatoclax significantly inhibited the migration of CT26 cells at concentrations as low as 0.01 µM. PMC10981831
IPSC-derived neurons with P525L FUS-eGFP 10 nM 24 hours Assessed p62 protein levels and found that obatoclax reduced p62 levels, ameliorating defects in protein homeostasis. PMC10527391
IPSC-derived neurons with P525L FUS-eGFP 10 nM 24 hours Quantified cytoplasmic FUS levels via immunostaining and found that obatoclax significantly reduced cytoplasmic FUS levels. PMC10527391
IPSC-derived neurons with P525L FUS-eGFP 1, 10, 100, 1000, 10000 nM 24 hours Assessed cell viability and found that obatoclax at 10 nM significantly reduced the formation of FUS-eGFP-positive stress granules. PMC10527391
Human melanoma cells (Mel-RM and MM200) 100 nM to 1 μM 24 or 48 hours Obatoclax as a single agent at nanomolar concentrations was relatively ineffective in inducing apoptosis, but when combined with ER stress inducers like tunicamycin or thapsigargin, it markedly enhanced apoptotic cell death. PMC2735806
CT26 cells 30 µM to 0.3 µM 24, 48, and 72 hours To evaluate the inhibitory effect of Obatoclax on the proliferation of CT26 cells. Results showed that Obatoclax significantly inhibited the growth of CT26 cells at lower concentrations. PMC10981831
KG-1 0.5, 1, 2.5, 5, 10 μM 24-72 hours Obatoclax inhibited KG-1 cell growth and induced apoptosis. PMC4096127
OCI-AML3 0.5, 1, 2.5, 5, 10 μM 24-72 hours Obatoclax inhibited OCI-AML3 cell growth and induced apoptosis, accompanied by S/G2 cell cycle arrest. PMC4096127
U937 0.5, 1, 2.5, 5, 10 μM 24-72 hours Obatoclax inhibited U937 cell growth and induced apoptosis, accompanied by cytochrome C release. PMC4096127
HL-60 0.5, 1, 2.5, 5, 10 μM 24-72 hours Obatoclax inhibited HL-60 cell growth and induced apoptosis, accompanied by Bak release from Mcl-1 and Bim release from Bcl-2/Mcl-1. PMC4096127
Reh cells 100 nM 48 h GX15-070 induces LC3 conversion and caspase-3 cleavage in Reh cells, indicating apoptosis and autophagy. PMC3032343
Jurkat cells 100 nM 48 h GX15-070 induces LC3 conversion and caspase-3 cleavage in Jurkat cells, indicating apoptosis and autophagy. PMC3032343
HSB-2 cells 100 nM 48 h GX15-070 induces LC3 conversion and caspase-3 cleavage in HSB-2 cells, indicating apoptosis and autophagy. PMC3032343
Molt-4 cells 100 nM 48 h GX15-070 induces LC3 conversion and p62 degradation in Molt-4 cells, indicating autophagic cell death. PMC3032343
CCRF-CEM (CEM) T-ALL cells 100 nM 48 h GX15-070 induces caspase-3 and PARP cleavage, increases the Annexin V-positive population, indicating apoptosis. Additionally, GX15-070 induces LC3 conversion and p62 degradation, markers of autophagic cell death. PMC3032343
Mouse embryonic fibroblasts (WT and DKO) 500 nM 48 hours Obatoclax-induced apoptosis is dependent on BAX/BAK, but loss of BAX/BAK fails to rescue cells PMC3032298
H1975 NSCLC cells 500 nM 48 hours Obatoclax induces BAK activation and mitochondrial outer membrane permeabilization PMC3032298
KMCH cells 400 nM and above 48 hours Inhibition of colony formation PMC2831099
BDEneu cells 200 nM 48 hours Inhibition of colony formation, induction of apoptosis PMC2831099
Mz-ChA-1 cells 5-100 nM 48 hours Inhibition of colony formation, induction of apoptosis PMC2831099
HuCCT-1 cells 5-100 nM 48 hours Inhibition of colony formation, induction of apoptosis PMC2831099
Melanocytes 1 μM 48 hours Obatoclax did not induce significant apoptotic cell death in melanocytes (<10% apoptotic cells). PMC2735806
WiDr 0~400 nM 48 hours Obatoclax significantly reduced cell viability with an IC50 of 231.04±2.01 nM PMC7084590
LoVo 0~400 nM 48 hours Obatoclax significantly reduced cell viability with an IC50 of 283.82±3.46 nM PMC7084590
HCT 116 0~400 nM 48 hours Obatoclax significantly reduced cell viability with an IC50 of 89.96±1.68 nM PMC7084590
DLD-1 0~400 nM 48 hours Obatoclax significantly reduced cell viability with an IC50 of 257.19±1.46 nM PMC7084590
Caco-2-hACE2 330 nM 72 hours Evaluate the inhibitory effect of Obatoclax on SARS-CoV-2 pseudovirus entry PMC8843317
A549-hACE2 330 nM 72 hours Evaluate the inhibitory effect of Obatoclax on SARS-CoV-2 pseudovirus entry PMC8843317
Calu-3-hACE2 330 nM 72 hours Evaluate the inhibitory effect of Obatoclax on SARS-CoV-2 pseudovirus entry PMC8843317
HEK293T-hACE2 330 nM 72 hours Evaluate the inhibitory effect of Obatoclax on SARS-CoV-2 pseudovirus entry PMC8843317

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Fischer 344 rats Rat cholangiocarcinoma model Intravenous injection 1.5 mg/kg Once daily for 5 consecutive days Evaluate the anti-tumor effect of Obatoclax in vivo, results showed significant reduction in tumor size and prolonged survival PMC2831099
Nude mice Subcutaneous xenograft model of K1 cells Subcutaneous injection 10 mg/kg/day (single agent) or 20 mg/kg/day (combination therapy) Once daily for 21 days Obatoclax alone or in combination with Vemurafenib significantly inhibited the growth of subcutaneous xenografts of K1 cells, and the tumor volume of the combination therapy group was significantly smaller than that of the single-agent treatment group. PMC5381260
BALB/c mice CT26-Luc2 colorectal liver metastasis model Intravenous injection 2 mg/kg or 5 mg/kg Once daily for 13 days To evaluate the inhibitory effect of Obatoclax on colorectal liver metastasis. Results showed that Obatoclax significantly inhibited liver metastasis at doses of 2 mg/kg and 5 mg/kg. PMC10981831
Nude mice H82 SCLC xenograft model Intraperitoneal injection 3 mg/kg Every 3 days for 21 days Significant inhibition of SCLC tumor growth and reduction of Ki-67 proliferation marker PMC8285499
SCID mice A20 lymphoma model Intraperitoneal injection 3 mg/kg/day Five consecutive days Obatoclax in combination with VSV significantly inhibited A20 lymphoma tumor growth in vivo, reducing tumor volume by 80%. PMC2997588
Nu/Nu mice CHLA06-ATRT and BT37 orthotopic xenograft models IP or oral Obatoclax 6 mg/kg IP or 10 mg/kg oral, TAK-228 6 mg/kg oral Once a week, continuous treatment To evaluate the effect of Obatoclax and TAK-228 combination therapy on tumor growth and survival, results showed that combination therapy significantly slowed tumor growth and extended median survival. PMC9050713

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01150656 - Completed - -
NCT00438178 Hematological Malignancies Phase 1 Completed - United States, District of Col... More >>umbia Georgetown University Medical Center Washington, District of Columbia, United States, 20007 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Canada, Ontario Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT00360035 Myelofibrosis Phase 2 Completed - United States, District of Col... More >>umbia Georgetown University Medical Center Washington, District of Columbia, United States, 20007 United States, Florida James A. Haley Veterans Hospital Tampa, Florida, United States, 33612 United States, Georgia Emory University Atlanta, Georgia, United States, 30322 United States, Illinois The University of Chicago Chicago, Illinois, United States, 60637 United States, Massachusetts University of Massachusetts Medical Center Worcester, Massachusetts, United States, 01655 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Canada, Ontario Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT00724841 Metastatic Melanoma Phase 1 Phase 2 Terminated(Study terminated pr... More >>ematurely due to financial contraints.) Less << - United States, Pennsylvania ... More >> University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 Less <<
NCT00521144 Recurrent Small Cell Lung Canc... More >>er Unspecified Adult Solid Tumor, Protocol Specific Less << Phase 1 Phase 2 Completed - United States, Maryland ... More >> Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Hospital Baltimore, Maryland, United States, 21231 United States, New York Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 Less <<
NCT01238146 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 Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Splenic Marginal Zone Lymphoma Less << Phase 1 Phase 2 Withdrawn(No patients accrued.... More >>) Less << - United States, Ohio ... More >> Arthur G. James Cancer Hospital and Solove Research Institute at Ohio State University Medical Center Columbus, Ohio, United States, 43210 Less <<
NCT00521144 - Completed - -
NCT00719901 Refractory Multiple Myeloma ... More >> Stage I Multiple Myeloma Stage II Multiple Myeloma Stage III Multiple Myeloma Less << Phase 1 Phase 2 Terminated(This trial was term... More >>inated due to slow accrual and the drug supply of Obatoclax during the phase I; therefore, the phase II portion will never open.) Less << - United States, Minnesota ... More >> Mayo Clinic Rochester, Minnesota, United States, 55905 Less <<
NCT00413114 Myelodysplastic Syndromes Phase 2 Completed - -
NCT00405951 Lung Cancer Phase 1 Phase 2 Completed - United States, Arizona ... More >> Mayo Clinic College of Medicine Scottsdale, Arizona, United States, 85259 United States, California Tower Oncology Beverly Hills, California, United States, 90210 United States, District of Columbia Georgetown University Washington, District of Columbia, United States, 20007 United States, Florida H. Lee Moffitt Cancer Center Tampa, Florida, United States, 33612 United States, Maryland University of Maryland Baltimore, Maryland, United States, 21201 MedStar Research Institute Baltimore, Maryland, United States, 21225 United States, Texas Arlington Cancer Center Arlington, Texas, United States, 76012 Less <<
NCT01563601 Extensive-stage Small Cell Lun... More >>g Cancer Less << Phase 3 Withdrawn(Business Decision) January 2018 -
NCT00407303 Mantle-Cell Lymphoma Phase 1 Phase 2 Completed - United States, Georgia ... More >> NW Georgia Oncology Centers Marietta, Georgia, United States, 30060 United States, Illinois Northwestern University Feinberg School of Medicine Chicago, Illinois, United States, 60611 United States, New Jersey Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 United States, New York Roswell Park Medical Center Buffalo, New York, United States, 14263 United States, Wisconsin University of Wisconsin Madison, Wisconsin, United States, 53792 Less <<
NCT00359892 Hodgkin's Lymphoma Phase 2 Completed - United States, Texas ... More >> MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT00918931 - Terminated - -
NCT00719901 - Terminated(This trial was term... More >>inated due to slow accrual and the drug supply of Obatoclax during the phase I; therefore, the phase II portion will never open.) Less << - -
NCT00612612 B-cell Chronic Lymphocytic Leu... More >>kemia Leukemia Prolymphocytic Leukemia Refractory Chronic Lymphocytic Leukemia Stage I Chronic Lymphocytic Leukemia Stage II Chronic Lymphocytic Leukemia Stage III Chronic Lymphocytic Leukemia Stage IV Chronic Lymphocytic Leukemia Less << Phase 1 Terminated - United States, Massachusetts ... More >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 Less <<
NCT00918931 Leukemia Syst... More >>emic Mastocytosis Less << Phase 2 Terminated - United States, Texas ... More >> UT MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT00427856 Lymphoma, Follicular Phase 2 Completed - United States, New Jersey ... More >> The Cancer Center at Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 Less <<
NCT00600964 Chronic Lymphocytic Leukemia Phase 1 Completed - United States, California ... More >> University of CA- San Diego La Jolla, California, United States, 92093 United States, District of Columbia Lombardi Cancer Center Washington, District of Columbia, United States, 20007 United States, Pennsylvania Milton S Hershey Medical Center Penn State Cancer Institute Hershey, Pennsylvania, United States, 17033 United States, Texas UT MD Anderson Cancer Center Houston, Texas, United States, 77030 Canada, Ontario Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT00933985 Acute Leukemias of Ambiguous L... More >>ineage Acute Undifferentiated Leukemia Angioimmunoblastic T-cell Lymphoma Blastic Phase Chronic Myelogenous Leukemia Childhood Burkitt Lymphoma Childhood Chronic Myelogenous Leukemia Childhood Diffuse Large Cell Lymphoma Childhood Immunoblastic Large Cell Lymphoma Childhood Nasal Type Extranodal NK/T-cell Lymphoma Cutaneous B-cell Non-Hodgkin Lymphoma Hepatosplenic T-cell Lymphoma Intraocular Lymphoma Noncutaneous Extranodal Lymphoma Peripheral T-cell Lymphoma Recurrent Childhood Acute Lymphoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Recurrent Childhood Anaplastic Large Cell Lymphoma Recurrent Childhood Grade III Lymphomatoid Granulomatosis Recurrent Childhood Large Cell Lymphoma Recurrent Childhood Lymphoblastic Lymphoma Recurrent Childhood Small Noncleaved Cell Lymphoma Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma Recurrent Mycosis Fungoides/Sezary Syndrome Recurrent/Refractory Childhood Hodgkin Lymphoma Refractory Chronic Lymphocytic Leukemia Refractory Hairy Cell Leukemia Relapsing Chronic Myelogenous Leukemia Small Intestine Lymphoma Unspecified Childhood Solid Tumor, Protocol Specific Less << Phase 1 Terminated - -
NCT00684918 AML PHASE2 COMPLETED 2025-12-09 Northwestern University, Chica... More >>go, Illinois, 60611, United States|The University of Iowa, Iowa City, Iowa, 52242, United States|University of Kansas Medical Center Research Institute, Westwood, Kansas, 66205, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02115, United States|St. Joseph Mercy Hospital, Ann Arbor, Michigan, 48106, United States|University of Michigan Health System, Ann Arbor, Michigan, 48109, United States|Michigan State University - Breslin Cancer Center, Lansing, Michigan, 48910, United States|St. Vincent's Comprehensive Cancer Center, New York, New York, 10011, United States|Legacy Emanuel Hospital & Health Center, Portland, Oregon, 97210, United States|Penn State Hershey Cancer Institute-Clinical Trials Office, Hershey, Pennsylvania, 17033, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States|Benaroya Research Institute at Virginia Mason, Seattle, Washington, 98101, United States|Princess Margaret Hospital, Toronto, Ontario, M5G 2M9, Canada Less <<
NCT00538187 Adult Non-Hodgkin Lymphoma ... More >> 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 Less << Phase 1 Terminated - United States, California ... More >> City of Hope Medical Center Duarte, California, United States, 91010 Less <<
NCT00682981 Extensive-stage Small Cell Lun... More >>g Cancer Less << Phase 1 Phase 2 Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.15mL

0.63mL

0.32mL

15.75mL

3.15mL

1.58mL

31.51mL

6.30mL

3.15mL

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