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TAK-243

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InvivoChem Cat #: V4576

CAS #: 1450833-55-2Purity ≥98%

Description: TAK-243 (also known as MLN-7243; TAK243; AOB-87172) is a novel, potent and selective inhibitor of ubiquitin-like modifier activating enzyme 1 (UBA1; also named as ubiquitin-activating enzyme (UAE)) with potential anticancer activity. TAK-243 binds to and inhibits UAE, which prevents both protein ubiquitination and subsequent protein degradation by the proteasome. This results in an excess of proteins in the cells and may lead to endoplasmic reticulum (ER) stress-mediated apoptosis. This inhibits tumor cell proliferation and survival.

References: Oncotarget. 2018 Apr 17;9(29):20265-20281.; Blood 2017, 130:814.

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	Name: TAK-243 CAS#: 1450833-55-2 Chemical Formula: C19H20F3N5O5S2 Exact Mass: 519.0858 Molecular Weight: 519.5142
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Technical Information	Synonym: TAK-243, AOB 87172; MLN7243, TAK 243, AOB-87172, MLN-7243, TAK243, AOB87172, MLN 7243 IUPAC/Chemical 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 InChi Key: PUMGWJMQPGYZFC-IDCJVQTKSA-N InChi Code: InChI=1S/C19H20F3N5O5S2/c1-32-34(30,31)26-14-8-13(17(28)18(14)29)24-15-5-6-23-16-9-12(25-27(15)16)10-3-2-4-11(7-10)33-19(20,21)22/h2-7,9,13-14,17-18,24,26,28-29H,8H2,1H3/t13-,14+,17+,18-/m1/s1 SMILES Code: COS(=O)(=O)N[[email protected]]1C[[email protected]]([[email protected]@H]([[email protected]@H]1O)O)NC2=CC=NC3=CC(=NN23)C4=CC(=CC=C4)SC(F)(F)F

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In Vitro	TAK-243 (MLN7243) selectively kills a subset of cutaneous squamous cell carcinoma (cSCC) lines. squamous cell carcinoma transplant (SCCT) and SCCRDEBMet cells are the most susceptible to continuous treatment with TAK-243. SCCIC1Met cells are also selectively killed by an extended exposure to TAK-243. Death in SCCRDEBMet cells displays the greatest sensitivity to a pulse of TAK-243. MLN7243 can reduce the cellular level of ubiquitin conjugates. TAK-243 decreases UBA1 and UBA6 thioesters and thioesters of the UBA6 specific E2 UBE2Z/USE1[1]. TAK-243 displays preferential activity towards acute myeloid leukemia (AML) cells over normal hematopoietic cells. TAK-243 reduces growth and viability of human AML cell lines (OCI-AML2, TEX, U937 and NB4) in a concentration- and time-dependent manner with IC50 's ranging from 15-40 nM after treatment for 48 hours[2].
In Vivo	TAK-243 significantly delays tumor growth in mice (T/C=0.02) with no toxicity as evidenced by no changes in mouse body weight, serum chemistry, or organ histology. TAK-243 reduces primary AML tumor burden in both tested samples without toxicity[2].
Cell Assay	Normal keratinocytes (normal human keratinocytes (NHK) and recessive dystrophic epidermolysis bullosa keratinocytes (RDEBK)) and cSCC cell lines are seeded into 96 well plates and live cell number and cell death are analysed with an IncuCyte ZOOM real-time imager using the CellTox Green Cytotoxicity Assay. Relative EC50 values are determined using GraphPad Prism. For clonogenic assays cells are seeded into six well plates. Inhibitors (e.g., TAK-243; 0.01, 0.1, 1, and 10 μM) are added for the indicated times and then cells are maintained in drug-free medium for up to 2 weeks to allow colony formation. Colonies are fixed in 10% methanol, 10% acetic acid and stained with crystal violet[1].
Animal Protocol	Mice: The preclinical efficacy and toxicity of TAK-243 are assessed in mouse models of AML. OCI-AML2 cells are injected subcutaneously (sc) into SCID mice, and when tumors are palpable, mice are treated with TAK-243 (20 mg/kg sc twice weekly). As an additional model, primary AML cells from 2 patients are injected into the femurs of NOD-SCID mice. Two weeks after injection, mice are treated with TAK-243 (20 mg/kg sc twice weekly). After 3 weeks of treatment, mice ae sacrificed, and AML engraftment in the non-injected femur is measured by flow cytometry[2].
References	[1]. Preclinical comparison of proteasome and ubiquitin E1 enzyme inhibitors in cutaneous squamous cell carcinoma: the identification of mechanisms of differential sensitivity. Oncotarget. 2018 Apr 17;9(29):20265-20281. [2]. TAK-243 Is a Selective UBA1 Inhibitor That Displays Preclinical Activity in Acute Myeloid Leukemia (AML). Blood 2017, 130:814.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Purity ≥98%
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TAK-243 (also known as MLN-7243; TAK243; AOB-87172) is a novel, potent and selective inhibitor of ubiquitin-like modifier activating enzyme 1 (UBA1; also named as ubiquitin-activating enzyme (UAE)) with potential anticancer activity.

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