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Catalog: | HY-10358 |
Brand: | MCE |
CAS: | 1032350-13-2 |
MDL | MFCD14584463 |
---|---|
Molecular Weight | 480.39 |
Molecular Formula | C25H23Cl2N5O |
SMILES | O=C1N2C(C3=CC(C4=CC=CC=C4)=C(N=C3C=C2)C5=CC=C(C6(N)CCC6)C=C5)=NN1.Cl.Cl |
Akt1 8 nM (IC 50 ) |
Akt2 12 nM (IC 50 ) |
Akt3 65 nM (IC 50 ) |
MK-2206 dihydrochloride (MK-2206 (2HCl)) (0-10 μM; 72 and 96 hours) inhibits the nasopharyngeal carcinoma (NPC) cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 proliferation in dose- and time-dependent manner
[1]
.
MK-2206 dihydrochloride (0-10 μM; 24 and 48 hours) results in a dose-dependent increase in the percentage of cells in G0/G1 phase and a concomitant reduction of cell numbers in S phase in CNE-2 and HONE-1 cells
[3]
.
MK-2206 dihydrochloride (0-10 μM; 24 hours) attenuates phosphorylation levels of PRAS40 and S6 in a dose-dependent manner. MK-2206 does not effect phosphorylation of GSKα/β and AKT
[3]
.
MK-2206 dihydrochloride (0-10 μM; 24 hours) increases the appearance of LC3-II in CNE-2 cells dose-dependently. Microtubule-associated protein 1 LC3 is an essential autophagy protein
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [3]
Cell Line: | The NPC cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 |
Concentration: | 0.08, 0.16, 0.31, 0.63, 1.25, 2.5, 5, 10 μM |
Incubation Time: | 72 and 96 hours |
Result: | At 72 and 96 hours, the IC 50 values in CNE-1, CNE-2, and HONE-1 cell lines were 3-5 μM, and in SUNE-1, they were less than 1 μM. |
Cell Cycle Analysis [3]
Cell Line: | CNE-2 and HONE-1 cells |
Concentration: | 0.625, 1.25, 2.5, 5, 10 μM |
Incubation Time: | 24 or 48 hours |
Result: | Induced cell cycle arrest at G1 in a dose-dependent manner. |
Western Blot Analysis [3]
Cell Line: | SUNE-1 and CNE-2 cells |
Concentration: | 0.625, 1.25, 2.5, 5, 10 μM |
Incubation Time: | 24 hours |
Result: | Inhibited phosphorylation of AKT downstream targets. |
Cell Autophagy Assay [3]
Cell Line: | CNE-2 cells |
Concentration: | 0.625, 1.25, 2.5, 5, 10 μM |
Incubation Time: | 24 hours |
Result: | Induced autophagy. |
Both MK-2206 dihydrochloride (MK-2206 (2HCl)) doses (oral gavage; 480 mg/kg once a week and 240 mg/kg three times a week; for 2 weeks) can inhibit the growth of human CNE-2 xenografts in nude mice. No other obvious toxicity is observed in mice
[3]
.
MK-2206 dihydrochloride (orally; 120 mg/kg; alternate days; for 3 weeks) significantly inhibits tumor growth in 3-5 week old athymic nude mice with GEO colon carcinoma cells
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Four- to 6-week-old male BALB/c nude mice with CNE-2 xenografts [3] |
Dosage: | 240 mg/kg and 480 mg/kg |
Administration: | Oral gavage; 240 mg/kg for three times a week; 480 mg/kg for once a week; for 2 weeks |
Result: | Both doses inhibited the growth of human CNE-2 xenografts in nude mice. |
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT01369849 | National Cancer Institute (NCI) |
Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia
|
September 2011 | Phase 1|Phase 2 |
NCT01466868 | Centre Leon Berard|National Cancer Institute, France |
Diffuse Large B Cell Lymphoma
|
November 2011 | Phase 2 |
NCT01425879 | National Cancer Institute (NCI) |
Advanced Adult Hepatocellular Carcinoma|Localized Non-Resectable Adult Liver Carcinoma|Recurrent Adult Liver Carcinoma|Recurrent Gallbladder Carcinoma|Stage IV Distal Bile Duct Cancer|Stage IV Gallbladder Cancer|Unresectable Extrahepatic Bile Duct Carcinoma|Unresectable Gallbladder Carcinoma
|
April 2011 | Phase 2 |
NCT01349933 | National Cancer Institute (NCI) |
Recurrent Squamous Cell Carcinoma of the Nasopharynx|Stage IV Squamous Cell Carcinoma of the Nasopharynx
|
April 2011 | Phase 2 |
NCT01231919 | National Cancer Institute (NCI) |
Accelerated Phase Chronic Myelogenous Leukemia|Acute Leukemias of Ambiguous Lineage|Acute Myeloid Leukemia+Transient Myeloproliferative Disorder|Acute Undifferentiated Leukemia|Aggressive NK-cell Leukemia|Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative|Blastic Phase Chronic Myelogenous Leukemia|Blastic Plasmacytoid Dendritic Cell Neoplasm|Childhood Burkitt Lymphoma|Childhood Chronic Myelogenous Leukemia|Childhood Diffuse Large Cell Lymphoma|Childhood Grade III Lymphomatoid Granulomatosis|Childhood Immunoblastic Large Cell Lymphoma|Childhood Nasal Type Extranodal NK+T-cell Lymphoma|Chronic Eosinophilic Leukemia|Chronic Myelomonocytic Leukemia|Chronic Neutrophilic Leukemia|Chronic Phase Chronic Myelogenous Leukemia|Intraocular Lymphoma|Juvenile Myelomonocytic Leukemia|Mast Cell Leukemia|Myeloid+NK-cell Acute Leukemia|Noncutaneous Extranodal Lymphoma|Post-transplant Lymphoproliferative Disorder|Primary Central Nervous System Hodgkin Lymphoma|Primary Central Nervous System Non-Hodgkin Lymphoma|Progressive Hairy Cell Leukemia, Initial Treatment|Prolymphocytic Leukemia|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 Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides+Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Recurrent+Refractory Childhood Hodgkin Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Hairy Cell Leukemia|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Unspecified Childhood Solid Tumor, Protocol Specific|Waldenström Macroglobulinemia
|
January 2011 | Phase 1 |
NCT01319539 | National Cancer Institute (NCI) |
Estrogen Receptor Negative|Estrogen Receptor Positive|HER2+Neu Negative|HER2+Neu Positive|Progesterone Receptor Negative|Progesterone Receptor Positive|Stage IA Breast Cancer|Stage IB Breast Cancer|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Triple-Negative Breast Carcinoma
|
April 2011 | Phase 2 |
NCT01283035 | National Cancer Institute (NCI) |
Ovarian Sarcoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma
|
April 2011 | Phase 2 |
NCT01249105 | Dana-Farber Cancer Institute|Brigham and Women´s Hospital|Massachusetts General Hospital|Beth Israel Deaconess Medical Center|Memorial Sloan Kettering Cancer Center|University of California, Los Angeles|Merck Sharp & Dohme LLC |
Malignant Glioma
|
Phase 2 | |
NCT01235897 | University of California, San Francisco|Merck Sharp & Dohme LLC |
Advanced Solid Tumors|Tumors|Cancer
|
March 2011 | Phase 1 |
NCT01239355 | National Cancer Institute (NCI) |
Adult Hepatocellular Carcinoma|Advanced Adult Hepatocellular Carcinoma|Localized Non-Resectable Adult Liver Carcinoma|Recurrent Adult Liver Carcinoma
|
December 2010 | Phase 2 |
NCT00670488 | Merck Sharp & Dohme LLC |
Locally Advanced Tumors|Metastatic Solid Tumors|Cancer|Neoplasms
|
April 15, 2008 | Phase 1 |
NCT01147211 | National Taiwan University Hospital |
Non Small Cell Lung Cancer
|
September 2010 | Phase 1 |
NCT01243762 | Merck Sharp & Dohme LLC |
Neoplasms Malignant
|
November 22, 2010 | Phase 1 |
NCT01071018 | Merck Sharp & Dohme LLC |
Solid Tumors
|
February 2010 | Phase 1 |
NCT01306045 | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
Carcinoma, Non-Small-Cell Lung|Carcinoma, Small Cell Lung|Carcinoma, Thymic
|
February 8, 2011 | Phase 2 |
NCT01295632 | Merck Sharp & Dohme LLC |
Advanced Cancer
|
February 2011 | Phase 1 |
NCT01658943 | National Cancer Institute (NCI) |
Pancreatic Acinar Cell Carcinoma|Pancreatic Ductal Adenocarcinoma|Recurrent Pancreatic Carcinoma|Stage IV Pancreatic Cancer
|
August 2012 | Phase 2 |
NCT01281163 | National Cancer Institute (NCI) |
Estrogen Receptor Negative|Estrogen Receptor Positive|HER2+Neu Positive|Progesterone Receptor Negative|Progesterone Receptor Positive|Recurrent Breast Carcinoma|Stage IV Breast Cancer
|
January 2011 | Phase 1 |
NCT01253447 | National Cancer Institute (NCI) |
Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Recurrent Adult Acute Myeloid Leukemia
|
October 2010 | Phase 2 |
NCT01776008 | National Cancer Institute (NCI) |
Estrogen Receptor Positive|HER2+Neu Negative|Recurrent Breast Carcinoma|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer
|
January 2013 | Phase 2 |
NCT01240941 | Vanderbilt-Ingram Cancer Center |
Metastatic Breast Cancer
|
February 2011 | Phase 2 |
NCT01333475 | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
Colorectal Neoplasms
|
March 2011 | Phase 2 |
NCT01186705 | Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme LLC |
Colon Cancer|Rectal Cancer
|
August 2010 | Phase 2 |
NCT01294306 | National Cancer Institute (NCI) |
Adenosquamous Lung Carcinoma|Bronchioloalveolar Carcinoma|Large Cell Lung Carcinoma|Lung Adenocarcinoma|Recurrent Non-Small Cell Lung Carcinoma|Squamous Cell Lung Carcinoma
|
February 2011 | Phase 2 |
NCT01021748 | Merck Sharp & Dohme LLC|AstraZeneca |
Locally Advanced or Metastatic Solid Tumors
|
November 23, 2009 | Phase 1 |
NCT01307631 | National Cancer Institute (NCI) |
Endometrial Adenocarcinoma|Endometrial Adenosquamous Carcinoma|Endometrial Clear Cell Adenocarcinoma|Endometrial Serous Adenocarcinoma|Recurrent Uterine Corpus Carcinoma
|
March 2011 | Phase 2 |
NCT01248247 | M.D. Anderson Cancer Center|Merck Sharp & Dohme LLC|National Cancer Institute (NCI)|GlaxoSmithKline|Novartis |
Lung Cancer
|
June 2, 2011 | Phase 2 |
NCT01251861 | National Cancer Institute (NCI) |
Recurrent Prostate Carcinoma|Stage I Prostate Cancer AJCC v7|Stage IIA Prostate Cancer AJCC v7|Stage IIB Prostate Cancer AJCC v7|Stage III Prostate Cancer AJCC v7
|
December 23, 2010 | Phase 2 |
NCT01604772 | National Cancer Institute (NCI) |
Recurrent Oral Cavity Adenoid Cystic Carcinoma|Recurrent Salivary Gland Carcinoma|Salivary Gland Adenoid Cystic Carcinoma|Stage IVA Major Salivary Gland Cancer AJCC v7|Stage IVA Oral Cavity Adenoid Cystic Carcinoma AJCC v6 and v7|Stage IVB Major Salivary Gland Cancer AJCC v7|Stage IVB Oral Cavity Adenoid Cystic Carcinoma AJCC v6 and v7|Stage IVC Major Salivary Gland Cancer AJCC v7|Stage IVC Oral Cavity Adenoid Cystic Carcinoma AJCC v6 and v7
|
July 23, 2012 | Phase 2 |
NCT01344031 | National Cancer Institute (NCI) |
Estrogen Receptor Positive|Invasive Breast Carcinoma|Recurrent Breast Carcinoma|Stage IV Breast Cancer AJCC v6 and v7
|
April 21, 2011 | Phase 1 |
NCT01263145 | National Cancer Institute (NCI) |
Adult Solid Neoplasm|Recurrent Breast Carcinoma|Stage IV Breast Cancer
|
January 5, 2011 | Phase 1 |
NCT00963547 | Merck Sharp & Dohme LLC |
Advanced Solid Tumors|Breast Cancer
|
September 15, 2009 | Phase 1 |
NCT01042379 | QuantumLeap Healthcare Collaborative |
Breast Neoplasms|Breast Cancer|Breast Tumors|Angiosarcoma|TNBC - Triple-Negative Breast Cancer|HER2-positive Breast Cancer|HER2-negative Breast Cancer|Hormone Receptor Positive Tumor|Hormone Receptor Negative Tumor|Early-stage Breast Cancer|Locally Advanced Breast Cancer
|
March 1, 2010 | Phase 2 |
NCT01260701 | National Cancer Institute (NCI) |
Adenocarcinoma of the Gastroesophageal Junction|Diffuse Gastric Adenocarcinoma|Gastric Intestinal Type Adenocarcinoma|Gastric Mixed Adenocarcinoma|Recurrent Gastric Carcinoma
|
January 2011 | Phase 2 |
NCT01783171 | National Cancer Institute (NCI) |
Pancreatic Adenocarcinoma|Recurrent Pancreatic Carcinoma|Stage III Pancreatic Cancer AJCC v6 and v7|Stage IV Pancreatic Cancer AJCC v6 and v7|Unresectable Pancreatic Carcinoma
|
January 15, 2013 | Phase 1 |
NCT00848718 | Merck Sharp & Dohme LLC |
Locally Advanced, Metastatic Solid Tumors
|
March 17, 2009 | Phase 1 |
NCT01859182 | National Cancer Institute (NCI) |
Adenocarcinoma of the Gallbladder|Adenocarcinoma With Squamous Metaplasia of the Gallbladder|Adult Primary Cholangiocellular Carcinoma|Advanced Adult Primary Liver Cancer|Cholangiocarcinoma of the Extrahepatic Bile Duct|Localized Unresectable Adult Primary Liver Cancer|Metastatic Extrahepatic Bile Duct Cancer|Recurrent Adult Primary Liver Cancer|Recurrent Extrahepatic Bile Duct Cancer|Stage II Gallbladder Cancer|Stage IIIA Gallbladder Cancer|Stage IIIB Gallbladder Cancer|Stage IVA Gallbladder Cancer|Stage IVB Gallbladder Cancer|Unresectable Extrahepatic Bile Duct Cancer
|
January 2013 | Phase 2 |
NCT01277757 | National Cancer Institute (NCI) |
Recurrent Breast Carcinoma|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer
|
March 2011 | Phase 2 |
NCT01519427 | National Cancer Institute (NCI) |
Recurrent Melanoma|Stage IIIA Melanoma|Stage IIIB Melanoma|Stage IIIC Melanoma|Stage IV Melanoma
|
January 2012 | Phase 2 |
NCT01480154 | National Cancer Institute (NCI) |
Advanced Malignant Solid Neoplasm|Stage III Cutaneous Melanoma AJCC v7|Stage III Prostate Cancer AJCC v7|Stage III Renal Cell Cancer AJCC v7|Stage IIIA Cutaneous Melanoma AJCC v7|Stage IIIB Cutaneous Melanoma AJCC v7|Stage IIIC Cutaneous Melanoma AJCC v7|Stage IV Cutaneous Melanoma AJCC v6 and v7|Stage IV Prostate Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7
|
November 23, 2011 | Phase 1 |
NCT01802320 | National Cancer Institute (NCI) |
Colon Mucinous Adenocarcinoma|Colon Signet Ring Cell Adenocarcinoma|Rectal Mucinous Adenocarcinoma|Rectal Signet Ring Cell Adenocarcinoma|Recurrent Colon Carcinoma|Recurrent Rectal Carcinoma|Stage IIIA Colon Cancer|Stage IIIA Rectal Cancer|Stage IIIB Colon Cancer|Stage IIIB Rectal Cancer|Stage IIIC Colon Cancer|Stage IIIC Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer
|
March 2013 | Phase 2 |
NCT01245205 | National Cancer Institute (NCI) |
HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Unspecified Adult Solid Tumor, Protocol Specific
|
November 2010 | Phase 1 |
NCT01370070 | Chinese University of Hong Kong |
Recurrent Nasopharyngeal Carcinoma
|
July 2011 | Phase 2 |
NCT01705340 | National Cancer Institute (NCI) |
Adenocarcinoma of the Gastroesophageal Junction|HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Recurrent Esophageal Cancer|Recurrent Gastric Cancer|Stage IIIC Breast Cancer|Stage IIIC Esophageal Cancer|Stage IIIC Gastric Cancer|Stage IV Breast Cancer|Stage IV Esophageal Cancer|Stage IV Gastric Cancer
|
September 2012 | Phase 1 |
NCT01481129 | National Cancer Institute (NCI) |
Diffuse Large B Cell Lymphoma
|
December 2011 | Phase 2 |
NCT01239342 | National Cancer Institute (NCI) |
Metastatic Kidney Carcinoma|Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7
|
January 27, 2011 | Phase 2 |
NCT01169649 | Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme LLC |
PANCREAS|Neuroendocrine
|
July 2010 | Phase 2 |
NCT01258998 | National Cancer Institute (NCI) |
Adult Nasal Type Extranodal NK+T-cell Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|B-cell Adult Acute Lymphoblastic Leukemia|B-cell Chronic Lymphocytic Leukemia|Cutaneous B-cell Non-Hodgkin Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Hepatosplenic T-cell Lymphoma|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Noncutaneous Extranodal Lymphoma|Peripheral T-cell Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|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 Hodgkin Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Adult T-cell Leukemia+Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin 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 Mycosis Fungoides+Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Hairy Cell Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|T-cell Adult Acute Lymphoblastic Leukemia|T-cell Large Granular Lymphocyte Leukemia|Testicular Lymphoma|Waldenström Macroglobulinemia
|
December 2010 | Phase 2 |
Solid
Room temperature in continental US; may vary elsewhere.
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
DMSO : 16.67 mg/mL ( 34.70 mM ; ultrasonic and warming and heat to 70°C)
H 2 O : 3.57 mg/mL ( 7.43 mM ; ultrasonic and warming and heat to 60°C)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.0816 mL | 10.4082 mL | 20.8164 mL |
5 mM | 0.4163 mL | 2.0816 mL | 4.1633 mL |
10 mM | 0.2082 mL | 1.0408 mL | 2.0816 mL |
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