2. MAPK/ERK Pathway
  3. Raf
  4. Raf inhibitor 1

Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.

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

Raf inhibitor 1 Chemical Structure

Raf inhibitor 1 Chemical Structure

CAS No. : 1093100-40-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 95 In-stock
Solution
10 mM * 1 mL in DMSO USD 95 In-stock
Solid
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10 mg USD 140 In-stock
50 mg USD 410 In-stock
100 mg USD 610 In-stock
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Based on 3 publication(s) in Google Scholar

Other Forms of Raf inhibitor 1:

Raf inhibitor 1 Related Antibodies

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BRaf c-Raf Raf

  • Biological Activity

  • Purity & Documentation

  • References

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Description

Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.

IC50 & Target[1]

B-Raf

1 nM (Ki)

B-RafV600E

1 nM (Ki)

c-Raf

0.3 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
A-375 IC50
2 nM
Compound: 1
Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
[PMID: 27085672]
MIA PaCa-2 EC50
22 nM
Compound: 1
Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method
Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method
[PMID: 27085672]
In Vitro

Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. Raf inhibitor 1 (Compound 13) binds to and stabilizes B-Raf in a DFG-out, inactive conformation in which the ATP pocket is partially filled by Phe595 and Gly596 from the DFG motif. Raf inhibitor 1 (Compound 13) additionally exhibits low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities or alternatively to pan-Raf inhibition, including Raf dimers[1].

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

Raf inhibitor 1 Related Antibodies
Molecular Weight

478.94

Formula

C26H19ClN8
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=CC=C2C(C=CN=C2NC3=CC=C(Cl)C=C3)=C1NC4=NC=CC=C4C5=NC=NC6=C5N=CN6
Shipping

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

DMSO : 50 mg/mL (104.40 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 2.0879 mL 10.4397 mL 20.8794 mL
5 mM 0.4176 mL 2.0879 mL 4.1759 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.22 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0879 mL 10.4397 mL 20.8794 mL 52.1986 mL
5 mM 0.4176 mL 2.0879 mL 4.1759 mL 10.4397 mL
10 mM 0.2088 mL 1.0440 mL 2.0879 mL 5.2199 mL
15 mM 0.1392 mL 0.6960 mL 1.3920 mL 3.4799 mL
20 mM 0.1044 mL 0.5220 mL 1.0440 mL 2.6099 mL
25 mM 0.0835 mL 0.4176 mL 0.8352 mL 2.0879 mL
30 mM 0.0696 mL 0.3480 mL 0.6960 mL 1.7400 mL
40 mM 0.0522 mL 0.2610 mL 0.5220 mL 1.3050 mL
50 mM 0.0418 mL 0.2088 mL 0.4176 mL 1.0440 mL
60 mM 0.0348 mL 0.1740 mL 0.3480 mL 0.8700 mL
80 mM 0.0261 mL 0.1305 mL 0.2610 mL 0.6525 mL
100 mM 0.0209 mL 0.1044 mL 0.2088 mL 0.5220 mL
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Raf inhibitor 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:

Raf inhibitor 11093100-40-3Raf inhibitor1Raf inhibitor-1RafRaf kinasesInhibitorinhibitorinhibit

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