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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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C127191-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $97.90 | |
C127191-25mg | 25mg | In stock | $162.90 | |
C127191-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $271.90 | |
C127191-100mg | 100mg | In stock | $489.90 | |
C127191-250mg | 250mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,102.90 |
Synonyms | 7-((4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yl)oxy)-N-hydroxyheptanamide | AS-16955 | FT-0665231 | UNII-1A7Y9MP123 | BDBM50307768 | GTPL8894 | 7-[4-(3-ethynylanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyheptanamide | SDCCGSBI-0050427.P003 | (+/-) |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | CUDC-101 inhibits the erlotinib-resistant EGFR mutant T790M although its effects are incomplete with an Amax of ~60% of peak enzyme activity after inhibition. CUDC-101 treatment increases the acetylation of histone H3 and H4, as well as the acetylation of |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Histone deacetylase inhibitor |
Note | 50mg、10mg、100mg卖完停产,不再备货 |
Product Description | CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively. |
ALogP | 4 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 7-[4-(3-ethynylanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyheptanamide |
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INCHI | InChI=1S/C24H26N4O4/c1-3-17-9-8-10-18(13-17)27-24-19-14-22(21(31-2)15-20(19)25-16-26-24)32-12-7-5-4-6-11-23(29)28-30/h1,8-10,13-16,30H,4-7,11-12H2,2H3,(H,28,29)(H,25,26,27) |
InChi Key | PLIVFNIUGLLCEK-UHFFFAOYSA-N |
Canonical SMILES | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC=CC(=C3)C#C)OCCCCCCC(=O)NO |
Isomeric SMILES | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC=CC(=C3)C#C)OCCCCCCC(=O)NO |
PubChem CID | 24756910 |
Molecular Weight | 434.49 |
PubChem CID | 24756910 |
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ChEMBL Ligand | CHEMBL598797 |
BindingDB Ligand | 50307768 |
CAS Registry No. | 1012054-59-9 |
Enter Lot Number to search for COA:
Solubility | DMSO ≥40mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
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1. Cai X, Zhai HX, Wang J, Forrester J, Qu H, Yin L, Lai CJ, Bao R, Qian C. (2010) Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.. J Med Chem, 53 (5): (2000-9). [PMID:20143778] [10.1021/op500134e] |
2. Shimizu T, LoRusso PM, Papadopoulos KP, Patnaik A, Beeram M, Smith LS, Rasco DW, Mays TA, Chambers G, Ma A et al.. (2014) Phase I first-in-human study of CUDC-101, a multitargeted inhibitor of HDACs, EGFR, and HER2 in patients with advanced solid tumors.. Clin Cancer Res, 20 (19): (5032-40). [PMID:25107918] [10.1021/op500134e] |
3. Galloway TJ, Wirth LJ, Colevas AD, Gilbert J, Bauman JE, Saba NF, Raben D, Mehra R, Ma AW, Atoyan R et al.. (2015) A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma.. Clin Cancer Res, 21 (7): (1566-73). [PMID:25573383] [10.1021/op500134e] |