| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
BET family bromodomains: BRD2, BRD3, BRD4, and BRDT. GS-626510 is an orally bioavailable inhibitor of BET family bromodomains.
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| ln Vitro |
GS-626510 binds to BRD2/3/4 with Kd values of 0.59-3.2 nM. It blocks both BD1 and BD2 bromodomains with IC50 values of 83 nM and 78 nM, respectively. These data demonstrate high potency across all BET bromodomains tested. GS-626510 is orally bioavailable. The compound suppresses BET-dependent transcriptional programs, leading to downregulation of oncogenes such as MYC. GS-626510 has anticancer activity in preclinical models.
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| ln Vivo |
In vivo, GS-626510 is orally bioavailable. As a BET inhibitor, it shows antitumor activity in preclinical models by modulating gene expression, particularly downregulating MYC and other oncogenic transcription programs. A single-dose PK study in NSG mice confirmed dosing of 10 mg/kg. The compound has been investigated for its anticancer activity in hematological malignancies and solid tumors. Specific in vivo efficacy data including animal models, dosing regimens, and detailed results are available in the primary literature but not extensively detailed in public search results.
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| Enzyme Assay |
BET bromodomain binding is assessed using in vitro binding assays such as AlphaScreen, time-resolved fluorescence resonance energy transfer (TR-FRET), or fluorescence polarization with recombinant bromodomain proteins and a fluorescent tracer. Kd values are calculated from binding curves using nonlinear regression analysis. IC50 values are calculated from competition binding curves. Selectivity is evaluated by profiling against a panel of bromodomains and other epigenetic reader domains.
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| Cell Assay |
Cellular activity is evaluated in cancer cell lines, including hematological malignancies and solid tumor cell lines. Cells are treated with GS-626510 at various concentrations (typically 0.001-100 μM) for 24-72 hours. Cell proliferation is measured by MTT, MTS, or CellTiter-Glo assays. BRD target engagement is assessed by cellular thermal shift assays (CETSA) or NanoBRET (bioluminescence resonance energy transfer) using BRD4-NanoLuc fusion constructs. MYC and other BET target gene expression (e.g., BCL2, CCND1, CDK6) is measured by qRT-PCR or RNA-seq. Apoptosis is assessed by caspase-3/7 activation or Annexin V staining. Cell cycle distribution is analyzed by flow cytometry.
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| Animal Protocol |
In vivo efficacy is studied in mouse xenograft models of cancer, including leukemia and solid tumors. GS-626510 is administered orally at various doses (e.g., 10 mg/kg). Tumor growth is measured by caliper twice weekly and tumor volume is calculated. At study termination, tumors are excised and weighed. Pharmacodynamic markers including BRD target engagement (by CETSA or immunohistochemistry), MYC expression (by qRT-PCR or immunohistochemistry), and downstream target gene expression are assessed in tumor tissue. Pharmacokinetic parameters are measured in plasma and tumor tissue. Single-dose PK studies are conducted to determine optimal dosing regimens.
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| ADME/Pharmacokinetics |
GS-626510 has a molecular formula of C24H20N4O2 and a molecular weight of 396.44 g/mol. CAS Number: 1637770-13-8. It is orally bioavailable. The compound is a potent BET family bromodomains inhibitor. GS-626510 was developed by Gilead and represents a distinct chemotype with a unique ADME profile. A single-dose PK study confirmed dosing of 10 mg/kg in NSG mice. The compound is soluble in DMSO and should be stored at -20°C for long-term stability, protected from light and moisture.
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| Toxicity/Toxicokinetics |
Safety data for GS-626510 indicate it is a research compound for laboratory use only. As a BET inhibitor, it may have effects on cell proliferation, gene expression, and hematopoiesis. Specific toxicological profiles including acute toxicity, organ toxicity, genotoxicity, and reproductive toxicity are not extensively published. Standard laboratory safety practices should be followed during handling, including the use of personal protective equipment and adequate ventilation. The compound is for research use only and not for human therapeutic applications without appropriate regulatory approval. Consult the material safety data sheet (MSDS) for detailed safety information.
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| References | |
| Additional Infomation |
GS-626510 is a research tool compound for studying BET bromodomain biology and epigenetic regulation. It is not approved for clinical use. The compound has been investigated for cancer research due to its ability to inhibit BET bromodomains and modulate oncogene expression. GS-626510 was developed by Gilead and represents a distinct chemotype with a unique ADME profile. The compound's high potency across all BET bromodomains (Kd 0.59-3.2 nM) and oral bioavailability make it a valuable tool for in vivo studies of BET-dependent transcription and for validating BET bromodomains as therapeutic targets in oncology.
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| Molecular Formula |
C25H22N4O
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|---|---|
| Molecular Weight |
394.468385219574
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| Exact Mass |
394.179
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| CAS # |
1637770-13-8
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| PubChem CID |
86301666
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| Appearance |
White to off-white solid powder
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| LogP |
5.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
626
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(C)=C(C(C)=N1)C1C=C(C2=C(C)C=CC3C2=CC=CN=3)C2=C(C=1)NC(C1CC1)=N2
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| InChi Key |
KHQQNXFBTALTQF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H22N4O/c1-13-6-9-20-18(5-4-10-26-20)22(13)19-11-17(23-14(2)29-30-15(23)3)12-21-24(19)28-25(27-21)16-7-8-16/h4-6,9-12,16H,7-8H2,1-3H3,(H,27,28)
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| Chemical Name |
4-[2-cyclopropyl-7-(6-methylquinolin-5-yl)-3H-benzimidazol-5-yl]-3,5-dimethyl-1,2-oxazole
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| Synonyms |
GS626510 GS 626510 GS-626510
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~63.38 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (6.34 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 | 2.5350 mL | 12.6752 mL | 25.3505 mL | |
| 5 mM | 0.5070 mL | 2.5350 mL | 5.0701 mL | |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.5350 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.
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