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Purity: ≥98%
GDC-0927 (formerly known as SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective ER (estrogen receptor) antagonist/ER degrader (SERD) that causes tumor regression in xenograft models grown from ER+ BC patients. As of right now, GDC-0927 looks to be well-tolerated. PK exposure appears to support QD dosing, there is evidence of strong PD target engagement, and heavily pretreated patients with advanced or metastatic ER+ BC—including those with ESR1 mutations—show encouraging anti-tumor activity. The potential for GDC-0927, an oral active SERD of the next generation, to surpass GDC-0810 as the best-in-class SERD molecule is apparent. GDC-0927 specifically targets the estrogen receptor alpha (ERα), a receptor that is expressed in over 70% of breast cancer cases, making it a commonly targeted target for the illness.
| Targets |
Estrogen receptor
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| ln Vitro |
GDC-0927 (formerly known as SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective ER (estrogen receptor) antagonist/ER degrader (SERD) that causes tumor regression in ER+ BC patient-derived xenograft models. With PK exposure supporting QD dosing, evidence of strong PD target engagement, and encouraging anti-tumor activity in heavily pretreated patients with advanced or metastatic ER+ BC, including patients with ESR1 mutations, GDC-0927 appears to be well tolerated so far. A next-generation orally active SERD called GDC-0927 appears to have more potential than GDC-0810 to be the best SERD molecule in its class. GDC-0927 targets the estrogen receptor alpha (ERα), which is a popular target for the disease because it is expressed in more than 70% of breast cancers.
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| 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)[1].
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| Cell Assay |
GDC-0927 (formerly known as SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective ER (estrogen receptor) antagonist/ER degrader (SERD). GDC-0927 targets the estrogen receptor alpha (ER), which is a popular target for the disease because it is expressed in more than 70% of breast cancers.
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| References |
| Molecular Formula |
C28H28FNO4
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| Molecular Weight |
461.53
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| Exact Mass |
461.20
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| Elemental Analysis |
C, 72.87; H, 6.12; F, 4.12; N, 3.03; O, 13.87
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| CAS # |
1642297-01-5
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| Related CAS # |
(R)-GDC-0927;1642297-53-7;GDC-0927 Racemate;1443983-36-5
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| Appearance |
Solid powder
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| SMILES |
CC1=C([C@@H](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-NDEPHWFRSA-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/t28-/m0/s1
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| Chemical Name |
(2S)-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) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.51 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 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 (4.51 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 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 (4.51 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 | 2.1667 mL | 10.8335 mL | 21.6671 mL | |
| 5 mM | 0.4333 mL | 2.1667 mL | 4.3334 mL | |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1667 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02316509 | Completed | Drug: GDC-0927 | Breast Cancer | Genentech, Inc. | March 17, 2015 | Phase 1 |
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