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CCT 137690

  Cat. No.:  DC8776  
CCT 137690
Chemical Structure
1095382-05-0
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More than 5000 active chemicals with high quality for research!
Field of application
CCT 137690 is a potent inhibitor of Aurora kinases (IC50 values are 0.015, 0.019 and 0.025 μM at Aurora A, Aurora C and Aurora B respectively).
Chemicals PropertiesBiological activityHow to use itCOA & MSDSRelated productsDatasheet
Cas No.: 1095382-05-0
Chemical Name:
Synonyms: CCT-137690; CCT137690
SMILES: CN1CCN(C2=CC=C(C3=NC4=C(C(N5CCN(CC6=NOC(C)=C6)CC5)=C(C=N4)Br)N3)C=C2)CC1
Formula: C26H31BrN8O
M.Wt: 551.48
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:
Description: CCT 137690 is a potent inhibitor of Aurora kinases (IC50 values are 0.015, 0.019 and 0.025 μM at Aurora A, Aurora C and Aurora B respectively).in vitro: CCT137690 displays antiproliferative activity in a range of human tumor cell lines, including SW620 colon carcinoma cell and A2780 ovarian cancer cell with GI50 of 0.3 and o.14 μM, respectively. In addition, CCT137690 also inhibit the phosphorylation of histone H3. CCT137690 inhibits the major cytochrome P450 isoforms (CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP3A4) with IC50 greater than 10 μM. However, CCT137690 is a moderate inhibitor of the hERG ion-channel with IC50 of 3.0 μM. CCT137690 inhibits autophosphorylation of FLT3 and phosphorylation of its downstream targets STAT5 and p44/42 MAPK (Erk1/2). CCT137690 effectively inhibits the growth of human tumor cell lines of different origins with GI50 ranging from 0.005 to 0.47 μM. CCT137690 completely inhibits both Aurora A autophosphorylation at T288 and histone H3 phosphorylation at 0.5 μM. CCT137690 induces polyploidy, mitotic aberrations, and apoptosis in HCT116 cells. CCT137690 reduces MYCN levels and GSK3β phosphorylation in the KELLY neuroblastoma cell line. in vivo: CCT137690 inhibits growth of MYCN-induced neuroblastoma at a dose of 100 mg/kg. Additionally, CCT137690 achieves target modulation and potently inhibits the growth of subcutaneous MOLM-13 xenografts, with no obvious toxicity or loss of body weight. CCT137690 is highly orally bioavailable and inhibits the growth of SW620 colon carcinoma xenografts with no observed toxicities as defined by body weight loss.
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MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC44124 TAS-119 TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.
DC42290 Pro-Phe-Phe Pro-Phe-Phe is the most aggregation-prone tripeptide of natural amino acids. Pro-Phe-Phe forms unique helical-like sheets that mate via aromatic dry interfaces. Pro-Phe-Phe can be used for the design of modular super-helical self-assembling nanostructures.
DC42289 SP-96 SP-96 is a highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC).
DC40564 SP-96 SP-96 is a?highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC).
DC40329 Tripolin A Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively.
DC40272 Hesperadin hydrochloride Hesperadin hydrochloride is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin hydrochloride inhibits Aurora B with an IC50 of 250 nM.
DC8776 CCT 137690 CCT 137690 is a potent inhibitor of Aurora kinases (IC50 values are 0.015, 0.019 and 0.025 μM at Aurora A, Aurora C and Aurora B respectively).
DC11759 AKCI A small-molecule inhibitor that blocks the Aurora C/IκBα interaction (IC50=24.9 uM) and exerts antitumor activity in MDA-MB-231 breast cancer cells.
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