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PROTAC BRAF-V600E degrader-1 

Cat. No.: HY-137487
Handling Instructions

PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth.

For research use only. We do not sell to patients.

PROTAC BRAF-V600E degrader-1 Chemical Structure

PROTAC BRAF-V600E degrader-1 Chemical Structure

CAS No. : 2417296-84-3

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Description

PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth[1].

IC50 & Target[1]

BRAF-V600E

2 nM (Kd)

Braf

2.4 nM (Kd)

In Vitro

PROTAC BRAF-V600E degrader-1 (compound 23) (1 nM-10 μM; 72 h) inhibits the cell viability of A375 and HT-29[1].
PROTAC BRAF-V600E degrader-1 (1-1000 nM; 16 h or 0-24 h) inhibits p-ERK and BRAF-V600E protein in A375 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: A375 and HT-29
Concentration: 1 nM-10 μM
Incubation Time: 72 h
Result: Inhibited the cell viability of A375 and HT-29 with IC50s of 46.5 nM and 51 nM.

Western Blot Analysis[1]

Cell Line: A375
Concentration: 1, 4, 12, 37, 111, 333 and 1000 nM
Incubation Time: 16 h or 0-24 h
Result: Induced the reduction in the phosphorylation of ERK.
Inhibited p-ERK and BRAF-V600E in a dose- and time-dependent manner.
Molecular Weight

1001.07

Formula

C48H54F2N10O10S

CAS No.
SMILES

CCCS(=O)(NC1=CC=C(F)C(N2C=C(C3=CN=CN=C3)C4=NC(N(C5CCN(C(CCOCCOCCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)CC5)C)=CC=C42)=C1F)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
PROTAC BRAF-V600E degrader-1
Cat. No.:
HY-137487
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