| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 62 nM (BRAF V600E kinase assay), 18 nM (Cell-Based Phosho-ERK Assay)[1].
Pan-RAF (including BRAF, BRAF-V600E, CRAF) |
|---|---|
| ln Vitro |
In various cancer cell lines, BAP-001 (Synthesis 13) displays 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 490 nM (RPMI8226].
TBAP-001 is a pan-RAF kinase inhibitor with an IC₅0 of 62 nM in the BRAF V600E kinase assay. In a cell‑based phospho‑ERK assay, it exhibits an IC₅0 of 18 nM, demonstrating potent inhibition of the MAPK signaling pathway. It is a potent inhibitor of the RAF/MEK/ERK pathway. |
| ln Vivo |
No detailed in vivo activity data for TBAP-001 has been reported. As a pan-RAF inhibitor, it is expected to suppress tumor growth in BRAF-mutant melanoma xenografts and potentially overcome resistance mechanisms associated with selective BRAF inhibitors.
|
| Enzyme Assay |
For non‑cellular assays, recombinant BRAF-V600E protein is incubated with TBAP-001 (0.1‑1000 nM) in the presence of ATP and a substrate (e.g., MEK). Kinase activity is measured by quantifying phosphorylated MEK via Western blotting, ELISA, or radiometric methods. IC₅0 values are calculated from dose‑response curves.
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| Cell Assay |
TBAP-001 is dissolved in DMSO and diluted in cell culture media (final DMSO ≤0.1%). BRAF‑V600E mutant melanoma cells (e.g., A375, SK-MEL-28) are treated with TBAP-001 at concentrations ranging from 0.1 nM to 10 uM for 2‑24 h. pERK levels are measured by Western blotting or ELISA. Cell proliferation is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
No detailed in vivo protocol for TBAP-001 has been reported. Based on standard procedures for RAF inhibitors, the compound would be formulated in a suitable vehicle (e.g., 10% DMSO, 40% PEG400, 5% Tween 80) and administered orally or intraperitoneally to mice bearing BRAF‑V600E melanoma xenografts. Efficacy would be assessed by tumor growth inhibition and pERK levels.
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| ADME/Pharmacokinetics |
No PK data for TBAP-001 has been reported. As a small‑molecule pan‑RAF inhibitor, it is expected to have moderate oral bioavailability. Solubility in DMSO is up to 120 mg/mL. Detailed parameters such as half‑life, Cmax, and clearance are not publicly available.
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| Toxicity/Toxicokinetics |
No toxicity data for TBAP-001 has been reported. As a pan‑RAF inhibitor, potential toxicities may include skin rash, hyperkeratosis, gastrointestinal effects, and paradoxical activation of the MAPK pathway in certain cellular contexts. No toxicology studies have been published.
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| References | |
| Additional Infomation |
The pan-RAF kinase inhibitor CCT3833 is an orally administered Raf inhibitor belonging to the serine/threonine protein kinase family, including A-Raf, B-Raf, and C-Raf, with potential antitumor activity. After administration, CCT3833 inhibits Raf-mediated signal transduction pathways, thereby suppressing the proliferation of Raf-overexpressing tumor cells. Raf protein kinases play a crucial role in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase (ERK) signaling pathway, which is frequently aberrantly activated in human cancers and plays a vital role in tumor cell proliferation and survival.
TBAP-001 (BAL3833; CAS: 1777832-90-2; formula: C2₇H23F2N₇O3; MW: 531.51) is a pan‑RAF kinase inhibitor extracted from patent WO2015075483A1. It is a research‑use compound with no reported clinical trials or regulatory approvals. It is soluble in DMSO and stable as a powder at ‑20degC. |
| Molecular Formula |
C27H23F2N7O3
|
|---|---|
| Molecular Weight |
531.513431787491
|
| Exact Mass |
531.183
|
| CAS # |
1777832-90-2
|
| PubChem CID |
91799359
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
4.3
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
39
|
| Complexity |
918
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC1=CC=CC(=C1)N1C(=CC(C(C)(C)C)=N1)NC(NC1C=CC(=CC=1F)OC1C=CN=C2C=1N=CC(N2)=O)=O
|
| InChi Key |
AJFKKXIBHCRFJO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C27H23F2N7O3/c1-27(2,3)21-13-22(36(35-21)16-6-4-5-15(28)11-16)33-26(38)32-19-8-7-17(12-18(19)29)39-20-9-10-30-25-24(20)31-14-23(37)34-25/h4-14H,1-3H3,(H,30,34,37)(H2,32,33,38)
|
| Chemical Name |
1-[5-tert-butyl-2-(3-fluorophenyl)pyrazol-3-yl]-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 250 mg/mL (470.36 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (3.91 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (3.91 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1881 mL | 0.9407 mL | 1.8814 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT02437227
Conditions:Melanoma|CancerProducts are for research use only; We do not sell to patients
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