Dabrafenib [1195765-45-7]
Katalog-Nummer HY-14660-200mg
Size : 200mg
Marke : MedChemExpress
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Dabrafenib (GSK2118436A) est un inhibiteur compétitif de l'ATP de Raf avec des IC50s de 5 nM et 0,6 nM pour C-Raf et B-RafV600E, respectivement.
Dabrafenib (GSK2118436A) ist ein ATP-kompetitiver Inhibitor von Raf mit IC50-Werten von 5 nM und 0,6 nM für C-Raf bzw. B-RafV600E.
Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively.
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Dabrafenib Chemische Struktur
CAS. Nr. : 1195765-45-7
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- Western blot confirmed increased MAPK pathway activity in NEC-DUE2 cells when compared to NECDUE1. Treatment with PLX4032 (1 μM), Dabrafenib (100 nM), or GSK1120212 (100 nM) for 4 hours leads to decreased MAPK signaling in NEC-DUE2 cells. Lysates are immunoblotted for the proteins indicated.
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| Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively. | ||||||||||||||||
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| In Vitro | Dabrafenib (GSK2118436, 1 μM) with 0.01 μM GSK1120212 inhibits more than 90% of cell growth in the NRAS mutant clones. GSK2118436 is sufficient to reduce S6P phosphorylation in A375. Dabrafenib suppresses the PolyP-mediated vascular barrier permeability, upregulation of inflammatory biomarkers, adhesion/migration of leukocytes, and activation and/or production of nuclear factor-κB, tumor necrosis factor-α, and interleukin-6. Dabrafenib inhibits the release of HMGB1 and downregulates HMGB1-dependent inflammatory responses by enhancing the expressions of cell adhesion molecules (CAMs) in human endothelial cells. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. | |||||||||||||||
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| In Vivo | Dabrafenib-treated females have mostly immature reproductive tracts with no evidence of ovulation, similar to age-matched controls; however, DAB-treated females have keratinized and histologically open vaginas. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. | |||||||||||||||
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| 519.56 | ||||||||||||||||
| C23H20F3N5O2S2 | ||||||||||||||||
| 1195765-45-7 | ||||||||||||||||
| Solid | ||||||||||||||||
| White to off-white | ||||||||||||||||
| CC(C)(C)C1=NC(C2=C(F)C(NS(C3=C(F)C=CC=C3F)(=O)=O)=CC=C2)=C(C4=CC=NC(N)=N4)S1 | ||||||||||||||||
Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
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| In Vitro: DMSO : ≥ 33 mg/mL (63.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) *"≥" means soluble, but saturation unknown. Preparing Stock Solutions
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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 and then sequentially add co-solvents:
In Vivo Dissolution Calculator Please enter the basic information of animal experiments: Dosage mg/kgAnimal weight Dosing volume 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 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. | ||||||||||||||||
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| For longer term proliferation assays, cells are plated and treated with compound or combination of compounds in RMPI-1640 containing 10% FBS for 12 days. Compound treatments are replaced at least once during the assay. After 12 days, cells are stained with 0.5% methylene blue in 50% ethanol. Images are captured using flatbed scanner. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz. |
| The rat pups selected as the test system are derived from 26 10-week-old, time-mated, virus-antibody-free SD (Crl:CD[SD]) female rats. Mated females are observed for natural deliveries from Day 20 to 23 pc (day parturition completed is designated PND 0). Litter examinations are conducted when parturition is complete, on PNDs 3 and 6, and included gender identification, individual pup weights, and external morphologic examinations. Parturient dams and their litters are selected for study based on clinical signs and body weights, and selected dams and their litters are randomized into study groups based on clinical observations and PND 3 litter mean body weights. On PND 3 or 4, litters are culled to four males and five females, with minimal fostering only when necessary to obtain the desired sex ratio, such that natural litters are maintained as much as possible. Records are kept of fostered pups of original and foster dams. All pups are identified by paw tattoo. To the extent possible, nonlittermates are assigned to subsets. DAB is formulated as a suspension in vehicle, 0.5% hydroxypropylmethylcellulose K15M, and 0.1% (v/v) Tween80 in purified water, and is given to juvenile male and female rats orally by gavage at a dose volume of 5 ml/kg, based on daily body weight. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz. |
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[1]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther, 2012, 11(4), 909-920.
[2]. Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22.
[3]. Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9.
[4]. Alexander M Menzies, et al. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012; 6: 391–405.
[5]. Posobiec LM, et al. Early Vaginal Opening in Juvenile Female Rats Given BRAF-Inhibitor Dabrafenib Is Not Associated with Early Physiologic Sexual Maturation. Birth Defects Res B Dev Reprod Toxicol. 2015 Dec;104(6):244-52.
* 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 |
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| DMSO | 1 mM | 1.9247 mL | 9.6235 mL | 19.2471 mL | 48.1176 mL |
| 5 mM | 0.3849 mL | 1.9247 mL | 3.8494 mL | 9.6235 mL | |
| 10 mM | 0.1925 mL | 0.9624 mL | 1.9247 mL | 4.8118 mL | |
| 15 mM | 0.1283 mL | 0.6416 mL | 1.2831 mL | 3.2078 mL | |
| 20 mM | 0.0962 mL | 0.4812 mL | 0.9624 mL | 2.4059 mL | |
| 25 mM | 0.0770 mL | 0.3849 mL | 0.7699 mL | 1.9247 mL | |
| 30 mM | 0.0642 mL | 0.3208 mL | 0.6416 mL | 1.6039 mL | |
| 40 mM | 0.0481 mL | 0.2406 mL | 0.4812 mL | 1.2029 mL | |
| 50 mM | 0.0385 mL | 0.1925 mL | 0.3849 mL | 0.9624 mL | |
| 60 mM | 0.0321 mL | 0.1604 mL | 0.3208 mL | 0.8020 mL |
- MAPK/ERK Pathway
- Raf
- 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:
Dabrafenib1195765-45-7GSK2118436A GSK2118436GSK2118436GSK 2118436GSK-2118436RafRaf kinasesInhibitorinhibitorinhibit
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