2. MAPK/ERK Pathway
  3. Raf
  4. TBAP-001

TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay.

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

TBAP-001 Chemical Structure

TBAP-001 Chemical Structure

CAS No. : 1777832-90-2

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 234 In-stock
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Based on 1 publication(s) in Google Scholar

TBAP-001 Related Antibodies

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  • Purity & Documentation

  • References

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Description

TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay[1].

IC50 & Target

IC50: 62 nM (BRAF V600E kinase assay), 18 nM (Cell-Based Phosho-ERK Assay)[1].
In Vitro

BAP-001 (Synthesis 13) exhibits IC50 values of 178 nM (A375), 62 nM (WM266.4), 72 nM (UACC62), 93 nM (LOX INVI), 590 nM (HT 29), 43 nM (COLO225), 690 nM (RKO), 490 nM (Mawi), 390 nM (WiDr), 480 nM (Colo741), 480 nM (SW620), 600 nM (HCT116), 390 nM (SKMEL2), 710 nM (D04), 390 nM (WM1361), 1150 nM (PDAC R172H (p53 mut)), 290 nM (MiaPaCa) and 490nM (RPMI8226) in different cancer cell lines[1].

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

TBAP-001 Related Antibodies
Molecular Weight

531.51

Formula

C27H23F2N7O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=CC(F)=C2)NC3=CC=C(OC4=C(N=C5)C(NC5=O)=NC=C4)C=C3F
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 : 250 mg/mL (470.36 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 1.8814 mL 9.4072 mL 18.8143 mL
5 mM 0.3763 mL 1.8814 mL 3.7629 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: 2.08 mg/mL (3.91 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 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 (20.8 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: 2.08 mg/mL (3.91 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 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 (20.8 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 1.8814 mL 9.4072 mL 18.8143 mL 47.0358 mL
5 mM 0.3763 mL 1.8814 mL 3.7629 mL 9.4072 mL
10 mM 0.1881 mL 0.9407 mL 1.8814 mL 4.7036 mL
15 mM 0.1254 mL 0.6271 mL 1.2543 mL 3.1357 mL
20 mM 0.0941 mL 0.4704 mL 0.9407 mL 2.3518 mL
25 mM 0.0753 mL 0.3763 mL 0.7526 mL 1.8814 mL
30 mM 0.0627 mL 0.3136 mL 0.6271 mL 1.5679 mL
40 mM 0.0470 mL 0.2352 mL 0.4704 mL 1.1759 mL
50 mM 0.0376 mL 0.1881 mL 0.3763 mL 0.9407 mL
60 mM 0.0314 mL 0.1568 mL 0.3136 mL 0.7839 mL
80 mM 0.0235 mL 0.1176 mL 0.2352 mL 0.5879 mL
100 mM 0.0188 mL 0.0941 mL 0.1881 mL 0.4704 mL
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TBAP-001 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:

TBAP-0011777832-90-2TBAP001TBAP 001RafRaf kinasesmelanomacolorectalcarcinomapancreaticlungInhibitorinhibitorinhibit

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