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Cat. No.: HY-137488

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PROTAC BRAF-V600E degrader-2

PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with K_ds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth.
(Pink: B-Raf^V600E ligand (HY-184546); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W074340)).

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

CAS No.: 2417296-82-1
Formula: C₄₂H₃₉F₂N₇O₈S
Molecular Weight:839.86

Storage:

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

Data Sheet (264 KB)

PROTAC BRAF-V600E degrader-2 Chemical Structure

CAS No.: 2417296-82-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with K_ds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth^[1]. (Pink: B-Raf^V600E ligand (HY-184546); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W074340)).

IC₅₀ & Target^[1]

BRAF-V600E

9.5 nM (Kd)

Braf

14.4 nM (Kd)

Cereblon

All PROTACs Isoforms :

All Raf Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	500 nM Compound: 12	Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay	[PMID: 32223235]
HT-29	IC₅₀	124 nM Compound: 12	Cytotoxicity in human HT-29 cells assessed as reduction in cell viability by Cell-titer-Lumi assay Cytotoxicity in human HT-29 cells assessed as reduction in cell viability by Cell-titer-Lumi assay	[PMID: 32223235]

Chemical Information

CAS No. 2417296-82-1
Molecular Weight 839.86
Formula C₄₂H₃₉F₂N₇O₈S
SMILES

O=C(NCC1=CC=C(C2=CN=C(NC=C3C(C4=C(F)C=CC(NS(=O)(CCC)=O)=C4F)=O)C3=C2)C=C1)CCCCNC5=CC6=C(C(N(C(CC7)C(NC7=O)=O)C6=O)=O)C=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (264 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Xiao-Ran Han, et al. Discovery of Selective Small Molecule Degraders of BRAF-V600E. J Med Chem. 2020 Apr 23;63(8):4069-4080. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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PROTAC BRAF-V600E degrader-2

All PROTACs Isoforms

All Raf Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC BRAF-V600E degrader-2 Related Classifications

HY-137488 Related Classifications