| Size | Price | |
|---|---|---|
| 100mg | ||
| Other Sizes |
Purity: ≥98%
| Targets |
ER-α (IC50 = 0.2 nM)
GDC-0927 Racemate targets the estrogen receptor (ER), specifically ER-α. As a selective estrogen receptor degrader (SERD), it binds to the estrogen receptor and promotes its degradation via the ubiquitin-proteasome pathway. This results in the complete elimination of ER signaling, which is critical for the growth of ER-positive breast cancer cells. The compound potently inhibits ER-α activity with an IC50 of 0.2 nM. |
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| ln Vitro |
GDC-0927 Racemate (Example 1) has an IC50 of 0.2 nM, is an agonist of the estrogen receptor, and is used in the study of ER-related disorders. It also potently inhibits ER-α activity. An IC50 of 0.21 nM is required for GDC-0927 Racemate to decrease MCF7 cell viability[1].
In vitro, GDC-0927 Racemate is a potent inhibitor of ER-α activity with an IC50 of 0.2 nM. As a SERD, it binds to the estrogen receptor and induces its degradation. The compound is non-steroidal and orally bioavailable, making it a promising candidate for research in ER-related diseases. Specific cellular assay data, such as EC50 values for receptor degradation, are not detailed in the available sources. |
| ln Vivo |
GDC-0927 is a novel, potent, non-steroidal, orally bioavailable, selective ER antagonist/ER degrader (SERD) that causes tumor regression in xenograft models of patients with estrogen receptor-positive breast cancer (ER+BC).
GDC-0927 Racemate causes tumor regression in xenograft models derived from ER+ breast cancer patients. This demonstrates significant in vivo antitumor activity against ER-positive breast cancer. As an orally bioavailable SERD, the compound offers the potential for convenient oral administration in therapeutic applications. Specific details of dosing regimens and efficacy data are not detailed in the available sources. |
| Enzyme Assay |
GDC-0927 (formerly known as SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective ER (estrogen receptor) antagonist/ER degrader (SERD), formerly known as SRN-927. Estrogen receptor alpha (ERα) is a popular target for breast cancer, and GDC-0927 targets this receptor, which is expressed in over 70% of cases of the disease.
The ER-α binding assay for GDC-0927 involves incubating the compound with recombinant ER-α protein and a fluorescent or radiolabeled estrogen ligand (such as [³H]-estradiol). After incubation, bound and free ligands are separated by a filtration or charcoal-dextran method. The radioactivity or fluorescence is measured, and the IC50 for displacement of the ligand is calculated. The compound's ability to induce ER degradation can be assessed by Western blot analysis of ER-α protein levels in treated cells. |
| Cell Assay |
To evaluate the cellular activity of GDC-0927, ER-positive breast cancer cell lines (such as MCF-7 or T47D cells) are seeded in 96-well plates and treated with varying concentrations of GDC-0927. Cell proliferation is measured using an MTT or SRB assay after 72 hours of treatment. ER-α protein levels are assessed by Western blot analysis to confirm degradation. Estrogen-responsive gene expression (such as pS2 or GREB1) is measured by quantitative RT-PCR to assess inhibition of ER signaling.
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| Animal Protocol |
The in vivo efficacy of GDC-0927 is evaluated in xenograft models using ER-positive breast cancer cell lines or patient-derived xenografts (PDX) from ER+ breast cancer patients. Tumor cells are implanted subcutaneously into immunodeficient mice. When tumors reach a certain size, mice are randomized into treatment groups and administered GDC-0927 orally at various doses. Tumor volume and body weight are measured twice weekly. Tumor regression is assessed by measuring the reduction in tumor volume relative to baseline. |
| ADME/Pharmacokinetics |
GDC-0927 is characterized as being orally bioavailable. Specific pharmacokinetic parameters (e.g., Cmax, Tmax, half-life, AUC) are not detailed in the available sources. The compound has a molecular weight of 461.52 and a molecular formula of C28H28FNO4. It is a small molecule with properties suitable for oral administration. As a powder, it is typically stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Specific toxicity data for GDC-0927 are not provided in the available sources. In xenograft studies, the compound caused tumor regression without mention of overt toxicity. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
GDC-0927 Racemate is also known as SRN-927 Racemate. It is a non-steroidal, orally bioavailable, selective estrogen receptor antagonist/degrader (SERD) that potently inhibits ER-α activity with an IC50 of 0.2 nM. It causes tumor regression in xenograft models derived from ER+ breast cancer patients and is used in the research of ER-related diseases.
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| Molecular Formula |
C28H28FNO4
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|---|---|---|
| Molecular Weight |
461.524631500244
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| Exact Mass |
461.2
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| CAS # |
1443983-36-5
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| Related CAS # |
GDC-0927;1642297-01-5;(R)-GDC-0927;1642297-53-7
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| PubChem CID |
71580895
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
703
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(OC2=C1C=C(C=C2)O)C3=CC=C(C=C3)OCCN4CC(C4)CF)C5=CC(=CC=C5)O
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| InChi Key |
KJAAPZIFCQQQKX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H28FNO4/c1-18-25-14-23(32)7-10-26(25)34-28(27(18)21-3-2-4-22(31)13-21)20-5-8-24(9-6-20)33-12-11-30-16-19(15-29)17-30/h2-10,13-14,19,28,31-32H,11-12,15-17H2,1H3
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| Chemical Name |
2-[4-[2-[3-(fluoromethyl)azetidin-1-yl]ethoxy]phenyl]-3-(3-hydroxyphenyl)-4-methyl-2H-chromen-6-ol
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1668 mL | 10.8338 mL | 21.6675 mL | |
| 5 mM | 0.4334 mL | 2.1668 mL | 4.3335 mL | |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1668 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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