PROTAC B-Raf degrader 1 - ≥99% , CAS No.2364367-27-9

CAS: 2364367-27-9 Cat. No.: P647574 Formula: C₃₆H₃₇N₅O₁₂S Peso molecolare: 763.77 PubChem CID: 138319681

GRADE & PURITY ≥99%

Storage

Store at -20°C,Argon charged

Shipped In

Ice chest + Ice pads

Application

PROTAC

Panoramica

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity

In Vitro

The IC 50 values of PROTAC B-Raf degrader 1 (compound 2) towards MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM, respectively. PROTAC B-Raf degrader 1 (5 or 10 μM) can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf. MCF-7 cells achieve an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation of PROTAC B-Raf degrader 1 with the concentration of 20 μM. PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cytotoxicity AssayCell Line: Human MCF-7 breast cancer cell line, MDA-MB-231 breast cancer cells, human HepG2 hepatoma cells, human normal LO2 liver cells, B16 cells. Concentration: 0-200 μM. Incubation Time: 72 hours. Result: The IC 50 values are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM in MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells, respectively. Western Blot AnalysisCell Line: Human MCF-7 breast cancer cell line. Concentration: 5 or 10 μM. Incubation Time: 24 hours. Result: Effectively induced the degradation of B-Raf and impacted the expression of Mcl-1. Apoptosis AnalysisCell Line: Human MCF-7 breast cancer cell line. Concentration: 2.7-20 μM. Incubation Time: 24 hours. Result: Achieved an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation with the concentration of 20 μM. Cell Cycle AnalysisCell Line: Human MCF-7 breast cancer cell line. Concentration: 20 μM. Incubation Time: 24 hours. Result: 1.94% cells were arrested at G1 phase, 8.20% at S phase, and 89.86% at G2/M phase.

Form:Solid

IC50& Target:B-Raf

Specifications

Specifiche e purezza

≥99%

Meccanismi biochimici e fisiologici

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.

Condizioni di conservazione di stoccaggio

Store at -20°C,Argon charged

Spedito in

Ice chest + Ice pads

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

INHIBITOR

Purezza

≥99%

Nomi e identificatori

Sorrisi canonici

COC1=C(C=C(C=C1)CS(=O)(=O)C=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)NCC(=O)NC3=CC=CC4=C3C(=O)N(C4=O)C5CCC(=O)NC5=O

IUPAC Name

N-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]-2-oxoethyl]-2-[2-methoxy-5-[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonylmethyl]anilino]acetamide

InChIKey

AMOFJSISJOOLNX-OUKQBFOZSA-N

INCHI

1S/C36H37N5O12S/c1-50-21-15-28(52-3)22(29(16-21)53-4)12-13-54(48,49)19-20-8-10-27(51-2)25(14-20)37-17-31(43)38-18-32(44)39-24-7-5-6-23-33(24)36(47)41(35(23)46)26-9-11-30(42)40-34(26)45/h5-8,10,12-16,26,37H,9,11,17-19H2,1-4H3,(H,38,43)(H,39,44)(H,40,42,45)/b13-12+

PubChem CID

138319681

Peso molecolare

763.77

Proprietà chimiche e fisiche

• Solubilità: DMSO : 25 mg/mL (32.73 mM; Need ultrasonic)

Domande frequenti

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C under argon. It is supplied under an argon blanket; reseal under inert gas after each use.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2364367-27-9, the molecular formula is C36H37N5O12S, and the molecular weight is 763.77 g/mol. InChIKey AMOFJSISJOOLNX-OUKQBFOZSA-N.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.