CB-839是Glutaminase(KGA和GAC)高效选择性、具口服活力抑制剂,对重组GAC的IC50值小于15nM。
CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.
1 mM
200 mg/kgp.o.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Gross MI, et al. Mol Cancer Ther. 2014, 13(4):890-901.
分子式 C26H24F3N7O3S |
分子量 571.57 |
CAS号 1439399-58-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02071927 | Acute Myeloid Leukemia (AML)|Acute Lymphocytic Leukemia (ALL) | Drug: CB-839|Drug: CB-Aza | Calithera Biosciences, Inc | Phase 1 | 2014-03-01 | 2017-02-07 |
NCT03047993 | Myelodysplastic Syndrome|Other Diseases of Blood and Blood-forming Organs | Drug: CB-839|Drug: Azacitidine | M.D. Anderson Cancer Center|National Cancer Institute (NCI)|Calithera Biosciences, Inc | Phase 1|Phase 2 | 2017-04-01 | 2017-02-06 |
NCT02944435 | Healthy Volunteers | Drug: CB-839 Capsules|Drug: CB-839 Tablets | Calithera Biosciences, Inc | Phase 1 | 2016-10-01 | 2017-01-03 |
NCT02071888 | Non-Hodgkin's Lymphoma (NHL)|Multiple Myeloma|Waldenstrom's Macroglobulinemia (WM)|Diffuse Large B-cell Lymphoma (DLBCL),|Other B-cell NHL Subtypes, Including WM|T-cell NHL | Drug: CB-839|Drug: CB-839 and low dose dexamethasone|Drug: CB-839, pomalidomide, and low dose dexamethasone | Calithera Biosciences, Inc | Phase 1 | 2014-02-01 | 2016-04-29 |
NCT02861300 | Colorectal Cancer|Colon Cancer|Rectal Cancer|Solid Tumor | Drug: CB-839|Drug: Capecitabine | Case Comprehensive Cancer Center | Phase 1|Phase 2 | 2016-08-01 | 2016-09-28 |
NCT02771626 | Clear Cell Renal Cell Carcinoma|Melanoma|Non-small Cell Lung Cancer | Drug: CB-839|Drug: Nivolumab | Calithera Biosciences, Inc | Phase 1|Phase 2 | 2016-08-01 | 2017-01-19 |
NCT02071862 | Solid Tumors|Triple-Negative Breast Cancer|Non Small Cell Lung Cancer|Renal Cell Carcinoma|Mesothelioma|Fumarate Hydratase (FH)-Deficient Tumors|Succinate Dehydrogenase (SDH)-Deficient Gastrointestinal Stromal Tumors (GIST)|Succinate Dehydrogenase (SDH)-Deficient Non-gastrointestinal Stromal Tumors|Tumors Harboring Isocitrate Dehydrogenase-1 (IDH1) and IDH2 Mutations|Tumors Harboring Amplifications in the cMyc Gene | Drug: CB-839|Drug: Pac-CB|Drug: CBE|Drug: CB-Erl|Drug: CBD|Drug: CB-Cabo | Calithera Biosciences, Inc | Phase 1 | 2014-02-01 | 2016-08-18 |
NCT03057600 | Triple Negative Breast Cancer|TNBC - Triple-Negative Breast Cancer | Drug: Pac-CB | Calithera Biosciences, Inc | Phase 2 | 2017-05-01 | 2017-02-17 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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