TAK-243 (MLN7243)

Name	methyl ((1S,2R,3S,4R)-2,3-dihydroxy-4-((2-(3-((trifluoromethyl)thio)phenyl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)cyclopentyl)sulfamate
Synonyms	TAK-243 MLN-7243 TAK-243 (MLN7243) methyl ((1S,2R,3S,4R)-2,3-dihydroxy-4-((2-(3-((trifluoromethyl)thio)phenyl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)cyclopentyl)sulfamate {(1R,2R,3S,4R)-2,3-Dihydroxy-4-[(2-{3-[(trifluoromethyl)sulfanyl]phenyl}pyrazolo[1,5-a]pyrimidin-7-yl)amino]cyclopentyl}methyl sulfamate Sulfamic acid, [(1R,2R,3S,4R)-2,3-dihydroxy-4-[[2-[3-[(trifluoromethyl)thio]phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]cyclopentyl]methyl ester
CAS	1450833-55-2

Molecular Formula	C19H20F3N5O5S2
Molar Mass	519.52
Density	1.75±0.1 g/cm3(Predicted)
pKa	9.35±0.70(Predicted)
Storage Condition	2-8°C(protect from light)
In vitro study	TAK-243 treatment resulted in depletion of cellular ubiquitination conjugates, resulting in disruption of signal transduction, induction of Protein toxicity stress, impaired cell cycle progression, and DNA damage repair pathways. TAK-243 has only a weak inhibitory effect on other closely related E1 ubiquitin-like activating enzymes, such as Fat10 activating enzyme, NEDD8 activating enzyme, SUMO activating enzyme, ISG15 activating enzyme and autophagy activating enzyme, its inhibitory activity was weaker than that of UAE. TAK-243 can inhibit the transfer of UAE ubiquitin to E2 enzyme. TAK-243 has an equally potent inhibitory effect on two E1 enzymes that activate ubiquitin (UBA6 and UAE). TAK-243 can significantly inhibit the UAE pathway downstream. However, TAK-243 treatment did not affect the protein levels of UAE(UBE1). A TAK-243 treatment can cause accumulation of short-lived proteins such as c-Jun, c-Myc, MCL1 and p53.
In vivo study	In a preliminary study of human xenografts, TAK-243 of the treatments resulted in the death of cancer cells. In a number of solid tumor and hematological tumor models, TAK-243 has a wide range of anti-tumor activity.

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Product Name: MLN7243 Visit Supplier Webpage Request for quotation
CAS: 1450833-55-2
Tel: 609-228-6898
Email: sales@medchemexpress.com
　　　　 tech@medchemexpress.com
Mobile: 609-228-6898

Spot supply

Product Name: TAK-243 Visit Supplier Webpage Request for quotation
CAS: 1450833-55-2
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922

Wechat: 18621343501
WhatsApp: +86-18621343501

Spot supply

Product Name: TAK-243 Visit Supplier Webpage Request for quotation
CAS: 1450833-55-2
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328

WhatsApp: +86-18821248368

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TAK-243 (MLN7243) Request for Quotation