2. PROTAC MAPK/ERK Pathway
  3. PROTACs Raf
  4. PROTAC BRAF-V600E degrader-1

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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Based on 1 publication(s) in Google Scholar

PROTAC BRAF-V600E degrader-1 Related Antibodies

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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].

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

PROTAC BRAF-V600E degrader-1 Related Antibodies

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.
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 170 mg/mL (169.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9989 mL 4.9947 mL 9.9893 mL
5 mM 0.1998 mL 0.9989 mL 1.9979 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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V2

In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9989 mL 4.9947 mL 9.9893 mL 24.9733 mL
5 mM 0.1998 mL 0.9989 mL 1.9979 mL 4.9947 mL
10 mM 0.0999 mL 0.4995 mL 0.9989 mL 2.4973 mL
15 mM 0.0666 mL 0.3330 mL 0.6660 mL 1.6649 mL
20 mM 0.0499 mL 0.2497 mL 0.4995 mL 1.2487 mL
25 mM 0.0400 mL 0.1998 mL 0.3996 mL 0.9989 mL
30 mM 0.0333 mL 0.1665 mL 0.3330 mL 0.8324 mL
40 mM 0.0250 mL 0.1249 mL 0.2497 mL 0.6243 mL
50 mM 0.0200 mL 0.0999 mL 0.1998 mL 0.4995 mL
60 mM 0.0166 mL 0.0832 mL 0.1665 mL 0.4162 mL
80 mM 0.0125 mL 0.0624 mL 0.1249 mL 0.3122 mL
100 mM 0.0100 mL 0.0499 mL 0.0999 mL 0.2497 mL
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PROTAC BRAF-V600E degrader-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC BRAF-V600E degrader-12417296-84-3PROTACsRafRaf kinasesanticancerBRAF-V600Eubiquitin-proteasome systemmelanomaA375HT-29Inhibitorinhibitorinhibit

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