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MLN2480

MLN2480

CAS: 1096708-71-2

Molecular Formula: C17H12Cl2F3N7O2S

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MLN2480 - Names and Identifiers

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

MLN2480 - Physico-chemical Properties

Molecular FormulaC17H12Cl2F3N7O2S
Molar Mass506.29
Density1.640
Melting Point197-199oC
Boling Point585.3±50.0 °C(Predicted)
Solubility DMSO (Slightly), Methanol (Slightly)
AppearanceSolid
ColorWhite
pKa10.07±0.46(Predicted)
Storage ConditionHygroscopic, Refrigerator, under inert atmosphere
In vitro studyMLN2480 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 studyMLN2480 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.

MLN2480 - Preparation solution concentration reference

 1mg5mg10mg
1 mM1.975 ml9.876 ml19.752 ml
5 mM0.395 ml1.975 ml3.95 ml
10 mM0.198 ml0.988 ml1.975 ml
5 mM0.04 ml0.198 ml0.395 ml
Last Update:2024-01-02 23:10:35

MLN2480 - Reference Information

biological activity MLN2480 (BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral Raf kinase inhibitor.
target TargetValue Raf
TargetValue
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
MLN2480
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Shanghai Amole Biotechnology Co., Ltd.
Spot supply
Product Name: MLN2480 Request for quotation
CAS: 1096708-71-2
Tel: 400-968-2212
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Shanghai Macklin Biochemical Co., Ltd
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CAS: 1096708-71-2
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
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SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
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Product Name: MLN2480 Visit Supplier Webpage Request for quotation
CAS: 1096708-71-2
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
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MedChemExpress (MCE)
Spot supply
Product Name: TAK-580; MLN 2480; BIIB-024 Visit Supplier Webpage Request for quotation
CAS: 1096708-71-2
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
Shanghai Yuanye Bio-Technology Co., Ltd.
Product Name: MLN2480 Visit Supplier Webpage Request for quotation
CAS: 1096708-71-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Shanghai Amole Biotechnology Co., Ltd.
Spot supply
Product Name: MLN2480 Request for quotation
CAS: 1096708-71-2
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
Shanghai Macklin Biochemical Co., Ltd
Spot supply
Product Name: MLN2480 Visit Supplier Webpage Request for quotation
CAS: 1096708-71-2
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: MLN2480 Visit Supplier Webpage Request for quotation
CAS: 1096708-71-2
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Spot supply
Product Name: TAK-580; MLN 2480; BIIB-024 Visit Supplier Webpage Request for quotation
CAS: 1096708-71-2
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
Shanghai Yuanye Bio-Technology Co., Ltd.
Product Name: MLN2480 Visit Supplier Webpage Request for quotation
CAS: 1096708-71-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
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MLN2480
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