RAF709|RAF-709|Raf kinase inhibitor
DC Chemicals, Website: www.dcchemicals.com
Product Name: RAF709|Cas Number: 1628838-42-5| Catalog Number: DC9987|Other Nmaes: RAF-709,RAF 709
RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
The invention provides compounds (e.g., RAF709) that inhibit Raf kinases, and are accordingly useful for treating certain disorders associated with excessive Raf kinase activity, including cell proliferation disorders such as cancers[1].
2017年11月15日星期三
SUN11602|SUN 11602| cas 704869-38-5
SUN11602|SUN 11602| cas 704869-38-5
DC Chemicals, Website: www.dcchemicals.com
Product Name: SUN11602|Cas Number: 704869-38-5| Catalog Number: DC10271|Other Nmaes: SUN11602，SUN11602
SUN11602 is a novel aniline compound, which mimics the neuroprotective mechanisms of basic fibroblast growth factor.
DC Chemicals, Website: www.dcchemicals.com
Product Name: SUN11602|Cas Number: 704869-38-5| Catalog Number: DC10271|Other Nmaes: SUN11602，SUN11602
SUN11602 is a novel aniline compound, which mimics the neuroprotective mechanisms of basic fibroblast growth factor.
Acebilustat(ZK322)|leukotriene A4 hydrolase inhibitor
Acebilustat(ZK322)|leukotriene A4 hydrolase inhibitor
DC Chemicals, Website: www.dcchemicals.com
Product Name: Acebilustat(ZK322)|Cas Number: 943764-99-6| Catalog Number: DC9986|Other Nmaes: ZK 322,ZK-322
Acebilustat(ZK322) is a potent and selective leukotriene A4 hydrolase inhibitor.
DC Chemicals, Website: www.dcchemicals.com
Product Name: Acebilustat(ZK322)|Cas Number: 943764-99-6| Catalog Number: DC9986|Other Nmaes: ZK 322,ZK-322
Acebilustat(ZK322) is a potent and selective leukotriene A4 hydrolase inhibitor.
OICR 9429|OICR9429|CAS 1801787-56-3
OICR 9429|OICR9429|CAS 1801787-56-3
DC Chemicals, Website: www.dcchemicals.com
Product Name: OICR9429|Cas Number: 1801787-56-3| Catalog Number: DC9985|Other Nmaes: OICR 9429,OICR 9429
OICR-9429 is a potent and selective chemical probe suitable to help dissect the biological role of WDR5 (Kdisp < 100 nM).
OICR-9429 is a potent and selective chemical probe suitable to help dissect the biological role of WDR5 (Kdisp < 100 nM).Exhibits selectivity for WDR5 over 22 methyltransferases and a panel of kinases, GPCRs, ion channels, and transporters. Reduces viability of acute myeloid leukemia cells in vitro. Also disrupts MLL1-RbBP5 interaction.
DC Chemicals, Website: www.dcchemicals.com
Product Name: OICR9429|Cas Number: 1801787-56-3| Catalog Number: DC9985|Other Nmaes: OICR 9429,OICR 9429
OICR-9429 is a potent and selective chemical probe suitable to help dissect the biological role of WDR5 (Kdisp < 100 nM).
OICR-9429 is a potent and selective chemical probe suitable to help dissect the biological role of WDR5 (Kdisp < 100 nM).Exhibits selectivity for WDR5 over 22 methyltransferases and a panel of kinases, GPCRs, ion channels, and transporters. Reduces viability of acute myeloid leukemia cells in vitro. Also disrupts MLL1-RbBP5 interaction.
E7449|E-7449|PARP1/PARP2 inhibitor
E7449|E-7449|PARP1/PARP2 inhibitor
DC Chemicals, Website: www.dcchemicals.com
Product Name: E-7449|Cas Number: 1140964-99-3| Catalog Number: DC9983|Other Nmaes: E7449,E 7449
E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2; enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors.
E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2; enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors.
E7449 is an orally bioavailable, potent, small molecule inhibitor of Poly(ADP-ribose) Polymerase (PARP)1 and PARP2. E7449 potently inhibits PARP1 and PARP2 in a cell-free assay and potentiates the cytotoxicity of both radiotherapy and chemotherapy. The cytotoxic effect of radiotherapy was enhanced by E7449 in clonogenic survival assays.
The anti-tumor activity of the alkylating agent temozolomide was potentiated by E7449 in a dose responsive manner in vivo in the B16-F10 melanoma isograft mouse model. Daily dosing of E7449 as a single agent significantly inhibited tumor growth in a genetically engineered BRCA1 null mouse ovarian xenograft model. In the BRCA1 mutant human breast cancer cell line MDA-MB-436, E7449 significantly inhibited proliferation in a long term growth inhibition assay in vitro. Oral administration of E7449 once daily potently inhibited tumor growth in the MDA-MB-436 xenograft model with no toxicity observed. A dose responsive pharmacodynamic effect on PARP activity was demonstrated in MDA-MB-436 tumor tissue following administration of a single E7449 dose. The decrease in PARP activity was sustained over several hours. The ability of E7449 to inhibit PARP activity in tumor tissue was further investigated in the H460 xenograft model. Following single oral administration of various E7449 dosages, inhibition of PARP activity in tumor tissue was determined over time. Studies revealed that PARP is inhibited by E7449 in a time and dose dependent manner with lower doses resulting in transient inhibition and higher doses causing more complete and sustained PARP inhibition. Conclusion: E7449 is a potent and selective PARP1 and PARP2 inhibitor with potent anti-tumor activity in BRCA-deficient in vivo models. It also potentiates the activity of radiotherapy and chemotherapy pre-clinically. Evaluation of E7449 in a Phase 1 study will be initiated soon.
DC Chemicals, Website: www.dcchemicals.com
Product Name: E-7449|Cas Number: 1140964-99-3| Catalog Number: DC9983|Other Nmaes: E7449,E 7449
E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2; enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors.
E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2; enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors.
E7449 is an orally bioavailable, potent, small molecule inhibitor of Poly(ADP-ribose) Polymerase (PARP)1 and PARP2. E7449 potently inhibits PARP1 and PARP2 in a cell-free assay and potentiates the cytotoxicity of both radiotherapy and chemotherapy. The cytotoxic effect of radiotherapy was enhanced by E7449 in clonogenic survival assays.
The anti-tumor activity of the alkylating agent temozolomide was potentiated by E7449 in a dose responsive manner in vivo in the B16-F10 melanoma isograft mouse model. Daily dosing of E7449 as a single agent significantly inhibited tumor growth in a genetically engineered BRCA1 null mouse ovarian xenograft model. In the BRCA1 mutant human breast cancer cell line MDA-MB-436, E7449 significantly inhibited proliferation in a long term growth inhibition assay in vitro. Oral administration of E7449 once daily potently inhibited tumor growth in the MDA-MB-436 xenograft model with no toxicity observed. A dose responsive pharmacodynamic effect on PARP activity was demonstrated in MDA-MB-436 tumor tissue following administration of a single E7449 dose. The decrease in PARP activity was sustained over several hours. The ability of E7449 to inhibit PARP activity in tumor tissue was further investigated in the H460 xenograft model. Following single oral administration of various E7449 dosages, inhibition of PARP activity in tumor tissue was determined over time. Studies revealed that PARP is inhibited by E7449 in a time and dose dependent manner with lower doses resulting in transient inhibition and higher doses causing more complete and sustained PARP inhibition. Conclusion: E7449 is a potent and selective PARP1 and PARP2 inhibitor with potent anti-tumor activity in BRCA-deficient in vivo models. It also potentiates the activity of radiotherapy and chemotherapy pre-clinically. Evaluation of E7449 in a Phase 1 study will be initiated soon.
I-CBP112|CBP/p300 bromodomain inhibitor
I-CBP112|CBP/p300 bromodomain inhibitor
DC Chemicals, Website: www.dcchemicals.com
Product Name: I-CBP112|Cas Number: 1640282-31-0| Catalog Number: DC9982|Other Nmaes: I-CBP112; I-CBP-112; I-CBP 112
I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.142 and 0.625 μM, respectively).
I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.142 and 0.625 μM, respectively). I-CBP112 has little activity against other bromodomains at concentrations up to 1 mM. I-CBP112 targets the CBP/p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. Interestingly, I-CBP112 increased the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.
DC Chemicals, Website: www.dcchemicals.com
Product Name: I-CBP112|Cas Number: 1640282-31-0| Catalog Number: DC9982|Other Nmaes: I-CBP112; I-CBP-112; I-CBP 112
I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.142 and 0.625 μM, respectively).
I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.142 and 0.625 μM, respectively). I-CBP112 has little activity against other bromodomains at concentrations up to 1 mM. I-CBP112 targets the CBP/p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. Interestingly, I-CBP112 increased the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.
TUG891|TUG-891|FFA4 (GPR120) agonist
TUG891|TUG-891|FFA4 (GPR120) agonist
DC Chemicals, Website: www.dcchemicals.com
TUG-891 is a potent and selective agonist of GPR120 with pEC50 values of 7.36 and 7.77 for human and mouse GPR120, respectively.
TUG-891 is a potent FFA4 (GPR120) agonist (pEC50 values are 7.36 and 7.77 for human and mouse GPR120 respectively). Selective for GPR120 over free fatty acid receptors (pEC50 = 4.19 for FFA1; displays no activity at FFA2 or FFA3). Cell permeable.
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