AU-15330

SKU: orb2900933

Description

AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.

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Key Properties

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CAS Number	2380274-50-8
MW	755.93
Purity	>98% (HPLC)
Formula	C₃₉H₄₉N₉O₅S
SMILES	C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](NC(=O)CN1CCN(CC1)c1cc(nnc1N)-c1ccccc1O)C(C)(C)C)c1ccc(cc1)-c1scnc1C
Solubility	In Vitro: DMSO : 140 mg/mL (185.20 mM; Ultrasonic )

Bioactivity

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In Vivo

Animal model: Six-week-old male CB17 severe combined immunodeficiency (SCID) mice. Dosage: 10 and 30 mg/kg. Administration: i. v. (5 days per week for 3 weeks). Result: Showed no evident toxicity in immuno-competent mice. Animal model: VCaP castration-resistant tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice). Dosage: 60 mg/kg with or without 10 mg/kg enzalutamide. Administration: i. v. (3 days per week); p.o. (5 days per week for 5 weeks). Result: Resulted inhibition of tumor growth and triggered disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals. Animal model: C4-2B non-castrated tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice). Dosage: 60 mg/kg with or without 30 mg/kg enzalutamide. Administration: i. v. (3 days per week); p.o. (5 days per week for 4 weeks). Result: Strongly inhibited the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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AU-15330 (orb2900933)

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Purity:	98.21% (May vary between batches)
CAS Number:	2380274-50-8
MW:	755.93
Formula:	C₃₉H₄₉N₉O₅S

CAS Number:	2380272-29-5
MW:	385.46
Formula:	C₂₀H₂₇N₅O₃

CAS Number:	2380275-40-9
MW:	755.93
Formula:	C₃₉H₄₉N₉O₅S

AU-15330

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

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AU-15330 (orb2900933)

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