| Identification | Back Directory | [Name]
(E)-3-(furan-2-yl)-N-[6-[[(E)-3-(furan-2-yl)prop-2-enoyl]amino]pyridin-2-yl]prop-2-enamide | [CAS]
1164471-33-3 | [Synonyms]
TT-012
2-Propenamide, N,N'-2,6-pyridinediylbis[3-(2-furanyl)-, (2E,2'E)-
(E)-3-(furan-2-yl)-N-[6-[[(E)-3-(furan-2-yl)prop-2-enoyl]amino]pyridin-2-yl]prop-2-enamide | [Molecular Formula]
C19H15N3O4 | [MDL Number]
MFCD00622207 | [MOL File]
1164471-33-3.mol | [Molecular Weight]
349.34 |
| Chemical Properties | Back Directory | [Boiling point ]
654.9±55.0 °C(Predicted) | [density ]
1.385±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
10.90±0.70(Predicted) | [color ]
Light yellow to brown |
| Hazard Information | Back Directory | [Biological Activity]
Potent and selective MITF dimerization disruptor with significant efficacy against melanoma both in vitro and in vivo.
TT-012 is a highly effective microphthalmia-associated transcription factor (MITF) dimerization inhibitor (Kd = 15.5 nM for the bHLH-LZ domain) th at specifically targets melanoma by disrupting MITFμs DNA-binding activity. TT012 exhibits notable potency in inhibiting MITF dimer formation (IC50 = 13.1 nM) and reducing the growth of B16F10 melanoma cells (IC50 = 499 nM)while also lowering mRNA levels of MITF target genes in these cells (IC50 < 3.12 μM). TT 012 is particularly effective against melanoma cells with elevated MITF expression and markedly diminishes tumor growth and pulmonary metastasis in miceachieving reductions of 79.7% and 93.9% at dosages of 2 mg/kg and 5 mg/kg respectivelycompared to controls. |
|
| Company Name: |
Henan Alfachem Co.,Ltd.
|
| Tel: |
0371-55051623 18137891487 |
| Website: |
https://www.chemicalbook.com/supplier/14555231/ |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|