1096708-71-2

Name	MLN2480
Synonyms	MLN2480 CS-2188 MLN 2480 MLN2480 BIIB-024 MLN-2480 MLN2480 (BIIB-024) (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide 6-Amino-5-chloro-N-[(1R)-1-[5-[[[5-chloro-4-(trifluoromethyl)-2-pyridinyl]amino]carbonyl]-2-thiazolyl]ethyl]-4-pyrimidinecarboxamide 2-[(1r)-1-[(6-amino-5-chloropyrimidine-4-carbonyl)amino]ethyl]-n-[5-chloro-4-(trifluoromethyl)pyridin-2-yl]-1,3-thiazole-5-carboxamide
CAS	1096708-71-2

Molecular Formula	C17H12Cl2F3N7O2S
Molar Mass	506.29
Density	1.640
Melting Point	197-199oC
Boling Point	585.3±50.0 °C(Predicted)
Solubility	DMSO (Slightly), Methanol (Slightly)
Appearance	Solid
Color	White
pKa	10.07±0.46(Predicted)
Storage Condition	Hygroscopic, Refrigerator, under inert atmosphere
In vitro study	MLN2480 inhibits the MAPK signaling pathway in clinical cancer models carrying BRAF and some RAS mutations. MLN2480 activates phosphorylated MEK at low concentrations, but inhibits this activity at high concentrations. The inhibitory effect of MLN2480 was all different in different models and Gene contexts. In an in vitro experiment, MLN2480 and TAK-733(MEK allosteric inhibitor) were used in combination in a cell proliferation assay, and the results demonstrate that these two small molecule compounds have synergistic activity. In addition, Western blot analysis demonstrated that MLN2480 inhibited negative feedback MEK activation due to TAK-733 treatment, thereby inhibiting the MAPK signaling pathway more effectively and consistently. The inhibitory effect of MLN2480 on PARK was weak.
In vivo study	MLN2480 has antitumor activity in xenograft models of melanoma, colon cancer, lung cancer, and pancreatic cancer. MLN2480(37.5 mg/kg) was well tolerated in a tumor xenograft model, MLN-2480(12.5 mg) versus TAK-733 (1 mg/kg). The combined use of is very effective in a SK-MEL-30 xenograft model, but the effect of its monotherapy is extremely weak.

Last Update：2024-01-02 23:10:35

biological activity	MLN2480 (BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral Raf kinase inhibitor.
target	TargetValue Raf
Target	Value
in vitro study	MLN2480 inhibit MAPK signaling pathway in clinical cancer models carrying BRAF and some RAS mutations. MLN2480 activated phosphorylated MEK at low concentrations, but inhibited this activity at high concentrations. The inhibitory effect of MLN2480 is also different under different models and gene backgrounds. In vitro experiments, MLN2480 and TAK-733(MEK allosteric inhibitor) were used in combination in cell proliferation detection. The results proved that these two small molecule compounds have synergistic activity. In addition, Western blot analysis proves that MLN2480 inhibits negative feedback MEK activation caused by TAK-733 processing, thus suppressing MAPK signal pathway more effectively and consistently. MLN2480 has a weaker inhibitory effect on PARK.
in vivo study	MLN2480 has anti-tumor activity in transplanted tumor models of melanoma, colon cancer, lung cancer and pancreatic cancer. MLN2480(37.5 mg/kg) is well tolerated in tumor xenograft models. The combination of MLN-2480(12.5 mg) and TAK-733 (1 mg/kg) is very effective in SK-MEL-30 transplanted tumor models, but its monotherapy is extremely weak.

Last Update：2024-04-09 21:54:55

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Product Name: MLN2480 Visit Supplier Webpage Request for quotation
CAS: 1096708-71-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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1096708-71-2

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