revisiondate:0 /2020 revisiondate:0 product data sheet ... · 2| applications: azd8330 decreased...

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1 | www.apexbt.com AZD8330 Cat. No.: A8374 CAS No.: 869357-68-6 Formula: C16H17FIN3O4 M.Wt: 461.23 Synonyms: ARRY-424704; ARRY-704; AZD-8330; ARRY424704; ARRY704; AZD8330 Target: MAPK Signaling Pathway: MEK1/2 Storage: Store at -20°C In Vitro ı23.05mg/mL in DMSO Preparing Stock Solutions Mass 1mg 5mg 10mg Solvent Concentration 1 mM 2.1681 mL 10.8406 mL 21.6812 mL 5 mM 0.4336 mL 2.1681 mL 4.3362 mL 10 mM 0.2168 mL 1.0841 mL 2.1681 mL Please refer to the solubility information to select the appropriate solvent. Shortsummary MEK 1/2 inhibitor IC₅₀ & Target 0.4 nM (ERK phosphorylation), 7 nM (MEK1/2) In Vitro Cell Viability Assay Cell Line: MOS, U2OS, KPD, ZK58, 143b and Saos-2 cells Preparation method˖ The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. Reacting conditions: 0 ~ 1 μM; 72 hrs Product Name: AZD8330 Revision Date: 0//2020 Product Data Sheet Solvent & Solubility Biological Activity 1 | www.apexbt.com AZD8330 Cat. No.: A837 7 7 7 7 7 7 7 7 7 4 4 4 4 4 4 4 4 4 4 4 CAS No.: 86 86 6 6 86 6 6 6 86 86 86 86 86 8 86 86 6 86 8 8 8693 93 93 93 93 93 93 93 93 9357 57 57 57 57 57 57 57 57 57 7 7 - - - - 68 6 6 6 6 6 6 6 6 6 6 6 - 6 Formula: C C1 C1 C1 C1 C1 C1 C1 C1 C C C C C C 6H17FIN3O4 M.Wt: 461.23 Synonyms: ARRY - Y Y 424704; ARRY - Y Y 704; AZ ZD - 8330; ARRY424704; ARRY704; AZD D8330 T arget: MAPK Signaling Pathway: MEK1/2 Storage: Store at - 20°C In Vitro ı 23.05mg/mL in DMSO Preparing Stock Solutions Mass 1mg 5mg 10mg Solvent Concentration 1 mM 2.1681 mL 10.8406 mL 21.6812 mL 5 mM 0.4336 mL 2.16 6 6 6 6 6 6 6 681 81 81 81 81 81 81 81 1 81 81 m m m m m m m m m m mL L L L L L L L L L 4.3362 mL 1 0 mM 0.2168 mL 1. 1. 1. 1. 1. . 1. 1. . 1.08 08 08 08 08 8 8 8 08 08 08 8 8 8 08 08 8 08 8 8 8 84 4 4 4 41 41 41 41 41 41 4 4 41 41 4 41 41 4 41 41 mL 2.1681 mL Pl Pl Pl Pl Pl Pl Pl Pl Pl Plea e e ea ea ea ea e ea e se se se se se se se se se se e se r r r r r r r r ref e e e e e er to the solubility information to select the appropriate s s s s s s s s s s s s sol ol ol ol ol ol ol ol ol ol ol ol ol o o ve ve ve ve ve e e ve ve e e e ve ve v ve ve v nt nt nt nt nt nt nt nt nt nt nt. . . Shortsummary MEK 1/2 inhibitor IC ₅₀ & Target 0.4 nM (ERK phosphorylation), 7 nM (MEK1/2) In Vitro Cell Viabi bi bi bi bi bi bi bi i bi b li li li li li li li li li l lity ty ty ty ty ty ty ty ty ty ty ty A A A A A A A A A A Ass ss ss ss ss ss ss ss ss ss s ss ss say a a a a a a a a a Ce Ce Ce Ce Ce e e Ce Ce e Cell l ll ll ll ll ll ll ll ll L L L L L L L L L L Lin in in in in in in in in i e: e: e: e: e: e e: e e e e e: e: e e e: e e: e e: e MOS, U2OS, KPD, ZK58, 143b and d d d d d d d d d d d S S S S S S S S S S S S Sao ao o o ao o o o a ao ao a a a s s s s s s s s s s s - - - - - - - - 2 2 2 2 2 2 2 2 2 2 2 2 ce c ce ce ce ce ce ce ce ce ce ce c ll l l l l s Pr Pr Pr Pr Pr Pr Pr Pr Pr P Pr rep ep ep ep ep ep ep ep ep ep epa a a ar a a a a a a a ation method ˖ The solubility of this compound in D D D D D D D D D D D D D DMS MS MS MS MS MS MS MS MS MS MS MS MS MS M MSO O O O O O O O O O O is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. Reacting conditions: 0 ~ 1 μM; 72 hrs Product Name: AZD8330 Revision Date: 0 / /2 020 0 et Product Data Shee Solvent & & & S S S S S S So o o o o ol l l lu u u u u u ub b b b b b bi i i i i il l l l l li i ity Biological Activity

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Page 1: RevisionDate:0 /2020 RevisionDate:0 Product Data Sheet ... · 2| Applications: AZD8330 decreased viability of MOS and U2OS cells, and significantly affected 143b cells. In contrast,

1 | www.apexbt.com

AZD8330Cat. No.: A8374

CAS No.: 869357-68-6

Formula: C16H17FIN3O4

M.Wt: 461.23

Synonyms: ARRY-424704; ARRY-704; AZD-8330;

ARRY424704; ARRY704; AZD8330

Target: MAPK Signaling

Pathway: MEK1/2

Storage: Store at -20°C

In Vitro

23.05mg/mL in DMSO

Preparing

Stock Solutions

Mass

1mg 5mg 10mgSolvent

Concentration

1 mM 2.1681 mL 10.8406 mL 21.6812 mL

5 mM 0.4336 mL 2.1681 mL 4.3362 mL

10 mM 0.2168 mL 1.0841 mL 2.1681 mL

Please refer to the solubility information to select the appropriate solvent.

Shortsummary MEK 1/2 inhibitor

IC₅₀ & Target 0.4 nM (ERK phosphorylation), 7 nM (MEK1/2)

In Vitro

Cell Viability Assay

Cell Line: MOS, U2OS, KPD, ZK58, 143b and Saos-2 cells

Preparation method The solubility of this compound in DMSO is >10 mM. General tips for obtaining

a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or

shake it in the ultrasonic bath for a while. Stock solution can be stored below -

20 °C for several months.

Reacting conditions: 0 ~ 1 μM; 72 hrs

Product Name: AZD8330Revision Date: 0 / /2020

Product Data Sheet

Solvent & Solubility

Biological Activity

1 | www.apexbt.com

AZD8330Cat. No.: A837777777777744444444444

CAS No.: 8686668666686868686868868668688869393939399393939393935757575757575757575777----6866666666666 -6

Formula: CC1C1C1C1C1C1C1C1CCCCCC 6H17FIN3O4

M.Wt: 461.23

Synonyms: ARRY-YY 424704; ARRY-YY 704; AZZD-8330;

ARRY424704; ARRY704; AZDD8330

Target: MAPK Signaling

Pathway: MEK1/2

Storage: Store at -20°C

In Vitro

23.05mg/mL in DMSO

Preparing

Stock Solutions

Mass

1mg 5mg 10mgSolvent

Concentration

1 mM 2.1681 mL 10.8406 mL 21.6812 mL

5 mM 0.4336 mL 2.1666666666818181818181818118181 mmmmmmmmmmmLLLLLLLLLL 4.3362 mL

10 mM 0.2168 mL 1.1.1.1.1..1.1..1.08080808088880808088880808808888844444141414141414441414414144141 mL 2.1681 mL

PlPlPlPlPlPlPlPlPlPleaeeeaeaeaeaeeae seseseseseseseseseseese rrrrrrrrrefeeeee er to the solubility information to select the appropriate sssssssssssssolololololololololololololoo veveveveveeeveveeeevevevvevev ntntntntntntntntntntnt...

Shortsummary MEK 1/2 inhibitor

IC₅₀ & Target 0.4 nM (ERK phosphorylation), 7 nM (MEK1/2)

In Vitro

Cell Viabibibibibibibibiibib lililililililililillitytytytytytytytytytytyty AAAAAAAAAAAssssssssssssssssssssssssssayaaaaaaaaa

CeCeCeCeCeeeCeCeeCelllllllllllllllllll LLLLLLLLLLLininininininininini e:e:e:e:e:ee:eeeee:e:eee:ee:ee:e MOS, U2OS, KPD, ZK58, 143b andddddddddddd SSSSSSSSSSSSSaoaoooaooooaaoaoaaa sssssssssss--------222222222222 ceccecececececececececec llllll s

PrPrPrPrPrPrPrPrPrPPrrepepepepepepepepepepepaaaaraaaaaaa ation method The solubility of this compound in DDDDDDDDDDDDDDMSMSMSMSMSMSMSMSMSMSMSMSMSMSMMSOOOOO OOOOOO is >10 mM. General tips for obtaining

a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or

shake it in the ultrasonic bath for a while. Stock solution can be stored below -

20 °C for several months.

Reacting conditions: 0 ~ 1 μM; 72 hrs

Product Name: AZD8330Revision Date: 0 / /20200

etProduct Data Shee

Solvent &&& SSSSSSSoooooolllluuuuuuubbbbbbbiiiiiilllllliiity

Biological Activity

Page 2: RevisionDate:0 /2020 RevisionDate:0 Product Data Sheet ... · 2| Applications: AZD8330 decreased viability of MOS and U2OS cells, and significantly affected 143b cells. In contrast,

2 | www.apexbt.com

Applications: AZD8330 decreased viability of MOS and U2OS cells, and significantly

affected 143b cells. In contrast, AZD8330 exhibited no effect on viability of

KPD, ZK58 and Saos-2 cells. According to a capase3/7 activity assay,

AZD8330 at the concentration of 0.5μM induced apoptosis in MOS and U2OS

cells, but not in KPD and ZK58 cells.

In VivoAnimal experiment

Applications:

1. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable

Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9.PMID:31063758

See more customer validations on www.apexbt.com.

[1]. Zuzanna Baranski, Tijmen H. Booij, Marieke L. Kuijjer, Yvonne de Jong, Anne-Marie Cleton-Jansen, Leo S. Price, Bob van de

Water, Judith V. M. G. Bovée, Pancras C.W. Hogendoorn, Erik H.J. Danen. MEK inhibition induces apoptosis in osteosarcoma cells

with constitutive ERK1/2 phosphorylation. Genes Cancer. 2015 Nov; 6(11-12): 503–512.

FOR RESEARCH PURPOSES ONLY.NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.Specific storage and handling information for each product is indicated on the product datasheet. Most APExBIO products are stable

under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage

temperature. Shortterm storage of many products are stable in the short-term at temperatures that differ from that required for

long-term storage. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt

of the product, follow the storage recommendations on the product data sheet.

APExBIO Technologywww.apexbt.com

7505 Fannin street, Suite 410, Houston, TX 77054. Tel: +1-832-696-8203 | Fax: +1-832-641-3177 | Email: [email protected]

Product Citations

References

Caution

2 | www.apexbt.com

Applications: AZD8330 decreased viability of MOS and U2OS cells, and significantly

affected 143b cells. In contrast, AZD8330 exhibited no effect on viability of

KPD, ZK58 and Saos-2 cells. According to a capase3/7 activity assay,

AZD8330 at the concentration of 0.5μM induced apoptosis in MOS and U2OS

cells, but not in KPD and ZK58 cells.

In VivoAnimal exxxxxxxxxxpepepepepepepepepepeepeririririririririririimememememememememememem ntntntntntntntntntntntntnttt

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1. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable

Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9.PMID:31063758

See more customer validations on www.apexbt.com.

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with constitutive ERK1/2 phosphorylation. Genes Cancer. 2015 Nov; 6(11-12): 503–512.

FOR RESEARCH PURPOSES ONLY.NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTTIC USE.Specific storage and handling informmmmmmmmatatatatatatatatatatataa ioioioioioioioioion for each product is indicatted on the product datasheet. Most AAAAAAAAAAAAAPEPEPEPEPEPEPEPEPPEEPPEExBxBxBxBxBxBxBxBxBBBBEEEEEE IOIOIOIOIOIOOIOOIOIOIOOOIOOO ble prpp oducts are stab

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temperature. Shortterm stststststststststsstorororororororororororagagagagagagagagaggggge eeeee e e ee eee eeeeeeeee oofofofofoofofofofofofofofofofoo mmmmmany products are stable in the sshort-term at temperaturesessssssessss tttttttthahahahahahahahahahhaat t t t tt t t tt t didididididididididiidididiffffffffffffffffffffffffff eeere from that required for

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APExBIO Teechnologywww.apexbt.comxbt com

7505 Fannin street, Suite 410, Houston, TX 77054.Tel: +1-832-696-8203 | Fax: +1-832-641-3177 | Email: [email protected]

Product Citations

References

Caution