Dabrafenib Mesylate
Based on 81 publication(s) in Google Scholar
Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 1195768-06-9
- Formula: C24H24F3N5O5S3
- Molecular Weight:615.67
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Dabrafenib Mesylate
More- Nature. 2026 Jan;649(8098):1032-1041. [Abstract]
- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Cancer Cell. 2024 Mar 11;42(3):358-377.e8. [Abstract]
- Cancer Cell. 2021 Aug 9;39(8):1135-1149.e8. [Abstract]
- Cancer Cell. 2020 Mar 16;37(3):387-402.e7. [Abstract]
- Cell. 2024 Jan 4;187(1):166-183.e25. [Abstract]
- Cell. 2018 Aug 9;174(4):843-855.e19. [Abstract]
- Cell Metab. 2025 May 6;37(5):1171-1188.e9. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Cell Res. 2025 Jan;35(1):23-44. [Abstract]
- Cancer Res. 2022 Jul 18;82(14):2552-2564. [Abstract]
- Mol Cell. 2019 Jan 3;73(1):7-21.e7. [Abstract]
- Nat Commun. 2025 Dec 17;16(1):11181. [Abstract]
- Nat Commun. 2025 May 8;16(1):4288. [Abstract]
- Cell Death Differ. 2022 Aug;29(8):1486-1499. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Adv Sci (Weinh). 2025 Aug 22:e08451. [Abstract]
- Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]
- Redox Biol. 2021 Oct:46:102110. [Abstract]
- J Control Release. 2024 Nov:375:643-653. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Cell Rep Med. 2024 Mar 19;5(3):101471. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- J Am Soc Nephrol. 2024 Jan 1;35(1):22-40. [Abstract]
- Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
- Phytomedicine. 2025 Oct:146:157151. [Abstract]
- Neoplasia. 2025 Oct:68:101223. [Abstract]
- Cell Syst. 2020 Nov 18;11(5):478-494.e9. [Abstract]
- Biomed Pharmacother. 2024 Jun 27:177:117033. [Abstract]
- J Transl Med. 2023 Jan 9;21(1):9. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2022;13(2):541-564. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- J Med Chem. 2025 Sep 25;68(18):19287-19302. [Abstract]
- Sci Signal. 2025 Sep 2;18(902):eadw3231. [Abstract]
- Elife. 2020 Dec 7;9:e61405. [Abstract]
- Mol Ther Nucleic Acids. 2024 Jul 19;35(3):102283. [Abstract]
- JCI Insight. 2023 Dec 22;8(24):e171140. [Abstract]
- JCO Precis Oncol. 2024 Apr:8:e2300538. [Abstract]
- Mol Cancer Ther. 2025 Dec 4. [Abstract]
- Mol Ther Oncolytics. 2019 Feb 5;12:235-245. [Abstract]
- Cells. 2019 Dec 6;8(12):1582. [Abstract]
- Int J Mol Sci. 2022 Nov 19;23(22):14385. [Abstract]
- Int J Cancer. 2019 Mar 15;144(6):1379-1390. [Abstract]
- RSC Adv. 2026 Jan 2;16(1):657-666. [Abstract]
- Toxicology. 2024 May:504:153807. [Abstract]
- Cell Rep Methods. 2026 Jun 15;6(6):101339. [Abstract]
- J Cell Mol Med. 2020 Mar;24(6):3336-3345. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Toxicol Appl Pharmacol. 2022 Jan 1:434:115797. [Abstract]
- Cancer Res Commun. 2026 Feb 16. [Abstract]
- Cancer Res Commun. 2024 Sep 1;4(9):2454-2462. [Abstract]
- Biophys J. 2018 Mar 27;114(6):1499-1511. [Abstract]
- Endocrine. 2025 Jan;87(1):220-233. [Abstract]
- Toxicol In Vitro. 2020 Jun;65:104777. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Cell Biochem Biophys. 2025 Mar;83(1):1113-1137. [Abstract]
- Biochem Biophys Rep. 2025 Sep 3:44:102235. [Abstract]
- Oncol Lett. 2025 Jul 18;30(4):450. [Abstract]
- Biochem Biophys Res Commun. 2020 Feb 5;522(2):395-401. [Abstract]
- Res Sq. 2026 Feb 18.
- bioRxiv. 2026 Jan 14.
- Res Sq. 2026 Jan 9.
- bioRxiv. 2025 Oct 13.
- Jagiellonian University. 2025.
- bioRxiv. 2025 Aug 25:2025.08.21.671520. [Abstract]
- University of Washington. 2025.
- Hong Kong Polytechnic University. 2025.
- Patent. US20240366605A1
- Patent. US20240366605A1.
- bioRxiv. 2024 Dec 20:2024.12.19.629301. [Abstract]
- Patent. US20240307400A1.
- bioRxiv. 2024 August 16.
- bioRxiv. 2023 Nov 13:2023.11.08.566316. [Abstract]
- Research Square Preprint. 2023 May 5.
- J Pers Med. 2022 Jan 8;12(1):77. [Abstract]
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
- bioRxiv. 2019 Oct.
- bioRxiv. 2019 Oct 28.
- bioRxiv. 2019 Sep.
- Oncotarget. 2017 Apr 4;8(14):23436-23447. [Abstract]
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Cell Proliferation/Viability Assay
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WB
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In Vivo Efficacy Study
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WB
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IF
Biological Activity
|
BRafV600E 0.6 nM (IC50) |
CRAF 5 nM (IC50) |
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[1]. 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[2]. 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[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1195768-06-9
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Appearance Solid
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Molecular Weight 615.67
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Formula C24H24F3N5O5S3
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Color White to off-white
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SMILES
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.CS(=O)(O)=O
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Synonyms
GSK2118436 Mesylate; GSK 2118436B
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (81)
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Journal Impact Factor
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Most Recent
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Nature
2026 Jan;649(8098):1032-1041. PMID: 41299171 -
Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Cancer Cell
2024 Mar 11;42(3):358-377.e8. PMID: 38215747 -
Cancer Cell
Evolutionary predictability of genetic versus nongenetic resistance to anticancer drugs in melanoma. [Abstract]2021 Aug 9;39(8):1135-1149.e8. PMID: 34143978 -
Cancer Cell
2020 Mar 16;37(3):387-402.e7. PMID: 32142667
Dabrafenib Mesylate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Mar 16;37(3):387-402.e7. [Abstract]
MCF-7 cells were seeded in 10-11 M E2 to which fulvestrant (F), dabrafenib (D), trametinib (T) or selumetinib (S) were subsequently added at 10-9, 10-6, 10-7 or 10-6 M, respectively. After 6 days, proteins were measured by immunoblotting, and phosphorylation levels (as defined by the levels of the phosphorylated form over total protein) relative to the vehicle-treated cells were set to 1.
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Cell
A TCF4-dependent gene regulatory network confers resistance to immunotherapy in melanoma. [Abstract]2024 Jan 4;187(1):166-183.e25. PMID: 38181739 -
Cell
2018 Aug 9;174(4):843-855.e19. PMID: 30017245 -
Cell Metab
2025 May 6;37(5):1171-1188.e9. PMID: 40037361 -
Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Cell Res
Tau is a receptor with low affinity for glucocorticoids and is required for glucocorticoid-induced bone loss. [Abstract]2025 Jan;35(1):23-44. PMID: 39743632 -
Cancer Res
Activity and Resistance of a Brain-Permeable Paradox Breaker BRAF Inhibitor in Melanoma Brain Metastasis. [Abstract]2022 Jul 18;82(14):2552-2564. PMID: 35584009 -
Mol Cell
2019 Jan 3;73(1):7-21.e7. PMID: 30472188 -
Nat Commun
Supporting cells orchestrate noise-induced hearing loss via a Gasdermin D-dependent signaling loop with hair cells. [Abstract]2025 Dec 17;16(1):11181. PMID: 41407982 -
Nat Commun
Structure-based design of potent and selective inhibitors targeting RIPK3 for eliminating on-target toxicity in vitro. [Abstract]2025 May 8;16(1):4288. PMID: 40341069 -
Cell Death Differ
2022 Aug;29(8):1486-1499. PMID: 35066575 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
2025 Aug 22:e08451. PMID: 40847444 -
Adv Sci (Weinh)
TRIM24 Cooperates with Ras Mutation to Drive Glioma Progression through snoRNA Recruitment of PHAX and DNA-PKcs. [Abstract]2024 Jun 3:e2400023. PMID: 38828688
Dabrafenib Mesylate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]
Inhibitory effects of Dabrafenib (40 µM; 24 h) on TRIM24 phosphorylation and protein interaction between TRIM24 and the DNA-PK complex in NHA/HRasV12/TRIM24 cells. Cells were treated with Dabrafenib for 24 h.
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Redox Biol
Inhibition of 6-formylindolo[3,2-b]carbazole metabolism sensitizes keratinocytes to UVA-induced apoptosis: Implications for vemurafenib-induced phototoxicity. [Abstract]2021 Oct:46:102110. PMID: 34418602 -
J Control Release
Confined copper depletion via a hydrogel platform for reversing dabrafenib/cetuximab resistance in BRAFV600E-mutant colorectal cancer. [Abstract]2024 Nov:375:643-653. PMID: 39306044 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Cell Rep Med
Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse. [Abstract]2024 Mar 19;5(3):101471. PMID: 38508142
Dabrafenib Mesylate purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Mar 19;5(3):101471. [Abstract]
Dabrafenib (30 mg/kg, p.o., 28 days). Relative tumor volumes and mice weights in sequential treatment groups with either vehicle or NEO2734 in A375 subcutaneous-bearing mice. Mice were switched to vehicle or NEO2734 treatment at day 28 (n = 6 for dabrafenib + trametinib to vehicle, n = 5 for dabrafenib + trametinib to NEO2734) (4 mg/kg NEO2734, 5 days/week; 30 mg/kg dabrafenib + 0.6 mg/kg trametinib daily).
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Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
J Am Soc Nephrol
2024 Jan 1;35(1):22-40. PMID: 37962623 -
Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
Phytomedicine
Parthenolide inhibits Hsp90α ATPase activity and overcomes acquired BRAF-inhibitor resistance in cutaneous melanoma. [Abstract]2025 Oct:146:157151. PMID: 40815947
Dabrafenib Mesylate purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct:146:157151. [Abstract]
Dabrafenib (20 μM; 24-48 h). Cell viability is assessed using CCK-8 assays. Dabrafenib (Dab) is used to treat BRAFi-resistant melanoma cells [WM164-DR] for 24 or 48 hours.
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Neoplasia
A methyl-to-acetyl switch in H3K27 drives metabolic reprogramming and resistance to BRAFV600E inhibition in melanoma. [Abstract]2025 Oct:68:101223. PMID: 40850308 -
Cell Syst
Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]2020 Nov 18;11(5):478-494.e9. PMID: 33113355
Dabrafenib Mesylate purchased from MedChemExpress. Usage Cited in: Cell Syst. 2020 Nov 18;11(5):478-494.e9. [Abstract]
Dabrafenib (25 mg/kg; p.o.; 5 days). Immunofluorescence microscopy of pERK in A375 mouse xenografts treated either with vehicle alone or dabrafenib plus trametinib for 5 days.
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Biomed Pharmacother
2024 Jun 27:177:117033. PMID: 38941889 -
J Transl Med
Papillary thyroid cancer organoids harboring BRAFV600E mutation reveal potentially beneficial effects of BRAF inhibitor-based combination therapies. [Abstract]2023 Jan 9;21(1):9. PMID: 36624452 -
Cell Mol Gastroenterol Hepatol
Recapitulating Cholangiopathy-Associated Necroptotic Cell Death In Vitro Using Human Cholangiocyte Organoids. [Abstract]2022;13(2):541-564. PMID: 34700031 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
J Med Chem
Synthesis and Structure-Activity Relationships of CRBN-Recruiting ZBTB11 Molecular Glue Degraders. [Abstract]2025 Sep 25;68(18):19287-19302. PMID: 40911408 -
Sci Signal
MAPK and mTORC1 signaling converge to drive cyclin D1 protein production to enable cell cycle reentry in melanoma persister cells. [Abstract]2025 Sep 2;18(902):eadw3231. PMID: 40892895 -
Elife
2020 Dec 7;9:e61405. PMID: 33284104 -
Mol Ther Nucleic Acids
Synthetic RIG-I agonist-mediated cancer immunotherapy synergizes with MAP kinase inhibition against BRAF-mutated melanoma. [Abstract]2024 Jul 19;35(3):102283. PMID: 39165562 -
JCI Insight
Dabrafenib protects from cisplatin-induced hearing loss in a clinically relevant mouse model. [Abstract]2023 Dec 22;8(24):e171140. PMID: 37934596 -
JCO Precis Oncol
Characterization of BRAFThr599dup Mutation as a Targetable Driver Mutation Identified in Lung Adenocarcinoma by Comprehensive Genomic Profiling. [Abstract]2024 Apr:8:e2300538. PMID: 38662982 -
Mol Cancer Ther
Mosperafenib, a novel paradox breaker BRAF inhibitor with potent preclinical activity in BRAF mutated colorectal cancer. [Abstract]2025 Dec 4. PMID: 41340484 -
Mol Ther Oncolytics
MAPK Inhibitors Enhance HDAC Inhibitor-Induced Redifferentiation in Papillary Thyroid Cancer Cells Harboring BRAF V600E: An In Vitro Study. [Abstract]2019 Feb 5;12:235-245. PMID: 30847387 -
Cells
B-RAFV600E Inhibitor Dabrafenib Attenuates RIPK3-Mediated Necroptosis and Promotes Functional Recovery after Spinal Cord Injury. [Abstract]2019 Dec 6;8(12):1582. PMID: 31817643 -
Int J Mol Sci
Dual Inhibition of BRAF-MAPK and STAT3 Signaling Pathways in Resveratrol-Suppressed Anaplastic Thyroid Cancer Cells with BRAF Mutations. [Abstract]2022 Nov 19;23(22):14385. PMID: 36430869 -
Int J Cancer
2019 Mar 15;144(6):1379-1390. PMID: 30144031
Dabrafenib Mesylate purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2019 Mar 15;144(6):1379-1390. [Abstract]
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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RSC Adv
Multifunctional Cu-DEOD porous polymeric nanocomposite for broad-spectrum biomedical applications. [Abstract]2026 Jan 2;16(1):657-666. PMID: 41488521 -
Toxicology
Decabromodiphenyl ether exposure reduces dabrafenib sensitivity of papillary thyroid carcinoma harboring BRAFV600E mutation through the EGFR-CRAF-MAPK pathway: An in vitro study. [Abstract]2024 May:504:153807. PMID: 38641160 -
Cell Rep Methods
Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]2026 Jun 15;6(6):101339. PMID: 42134319 -
J Cell Mol Med
Combined tazemetostat and MAPKi enhances differentiation of papillary thyroid cancer cells harbouring BRAFV600E by synergistically decreasing global trimethylation of H3K27. [Abstract]2020 Mar;24(6):3336-3345. PMID: 31970877 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Toxicol Appl Pharmacol
Dabrafenib inhibits ABCG2 and cytochrome P450 isoenzymes; potential implications for combination anticancer therapy. [Abstract]2022 Jan 1:434:115797. PMID: 34780725 -
Cancer Res Commun
BRAF V600E Expression in c-Kit+ Interstitial Cells of Cajal Drives Gastrointestinal Stromal Tumor Formation in Mice. [Abstract]2026 Feb 16. PMID: 41697759 -
Cancer Res Commun
2024 Sep 1;4(9):2454-2462. PMID: 39212544 -
Biophys J
2018 Mar 27;114(6):1499-1511. PMID: 29590606 -
Endocrine
POU5F1B is responsible for the acquired resistance to dabrafenib in papillary thyroid cancer cells with the BRAF V600E mutation. [Abstract]2025 Jan;87(1):220-233. PMID: 39136897 -
Toxicol In Vitro
Combined SRPK and AKT pharmacological inhibition is synergistic in T-cell acute lymphoblastic leukemia cells. [Abstract]2020 Jun;65:104777. PMID: 31962201 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
Cell Biochem Biophys
Mechanistic Regulation of Epidermal Growth Factor and Hormonal Receptors by Kinase Inhibitors and Organofluorines in Breast Cancer Therapy. [Abstract]2025 Mar;83(1):1113-1137. PMID: 39316263 -
Biochem Biophys Rep
OT17 a novel microsatellite stable colorectal cancer cell line and organoid model for investigating BRAF V600E mutant tumorigenesis and targeted therapeutics. [Abstract]2025 Sep 3:44:102235. PMID: 40978200 -
Oncol Lett
Identification of key ferroptosis-related genes associated with the development of gastric cancer: Prognostic models, molecular mechanisms and potential treatment strategies. [Abstract]2025 Jul 18;30(4):450. PMID: 40747376 -
Biochem Biophys Res Commun
Protective effect of dabrafenib on renal ischemia-reperfusion injury in vivo and in vitro. [Abstract]2020 Feb 5;522(2):395-401. PMID: 31771879 -
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bioRxiv
2025 Aug 25:2025.08.21.671520. PMID: 40909720 -
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bioRxiv
BRAFV600 and ErbB inhibitors directly activate GCN2 in an off-target manner to limit cancer cell proliferation. [Abstract]2024 Dec 20:2024.12.19.629301. PMID: 39763857 -
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bioRxiv
KSR1 knockout mouse model demonstrates MAPK pathway's key role in cisplatin- and noise-induced hearing loss. [Abstract]2023 Nov 13:2023.11.08.566316. PMID: 38014104 -
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J Pers Med
2022 Jan 8;12(1):77. PMID: 35055392 -
ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077 -
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Oncotarget
Parthenolide suppresses non-small cell lung cancer GLC-82 cells growth via B-Raf/MAPK/Erk pathway. [Abstract]2017 Apr 4;8(14):23436-23447. PMID: 28423582
Solvent & Solubility
DMSO : 20.83 mg/mL (33.83 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.06 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.06 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 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.
Please enter the basic information of animal experiments:
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-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
-
+%Tween-80 + +
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%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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[2]. Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22. [Content Brief]
[3]. Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9. [Content Brief]
[4]. Alexander M Menzies, et al. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012; 6: 391–405. [Content Brief]
[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. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.6242 mL | 8.1212 mL | 16.2425 mL | 40.6062 mL |
| 5 mM | 0.3248 mL | 1.6242 mL | 3.2485 mL | 8.1212 mL | |
| 10 mM | 0.1624 mL | 0.8121 mL | 1.6242 mL | 4.0606 mL | |
| 15 mM | 0.1083 mL | 0.5414 mL | 1.0828 mL | 2.7071 mL | |
| 20 mM | 0.0812 mL | 0.4061 mL | 0.8121 mL | 2.0303 mL | |
| 25 mM | 0.0650 mL | 0.3248 mL | 0.6497 mL | 1.6242 mL | |
| 30 mM | 0.0541 mL | 0.2707 mL | 0.5414 mL | 1.3535 mL |