AUR-1545 free base · Synonyms: AUR 1545 · AUR1545

AUR1545 is a selective KAT2A/KAT2B ((GCN5/PCAF)) PROTAC degrader that induces monocyte differentiation and inhibits the growth of acute myeloid…

For research use only. Not for human or veterinary use.

Target PROTACs Histone Acetyltransferase

Research area Cancer

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Data Sheet SDS COA

AUR-1545 structure

CAS No.: 3031593-79-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 995.00	BP-02276-50mg	In stock	Get quote
100 mg	USD 1,680.00	BP-02276-100mg	In stock	Get quote
250 mg	USD 2,985.00	BP-02276-250mg	In stock	Get quote
500 mg	Inquire	BP-02276-500mg	In stock	Inquire
1 g	Inquire	BP-02276-1g	In stock	Inquire

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Description

AUR1545 is a selective KAT2A/KAT2B ((GCN5/PCAF)) PROTAC degrader that induces monocyte differentiation and inhibits the growth of acute myeloid leukemia cells. AUR1545 inhibits cell growth, induces epithelial differentiation and suppresses tumor growth in small cell lung cancer models. AUR1545 inhibits cell growth and induces differentiation in neuroendocrine prostate cancer cells and primary patient-derived organoids. AUR1545 is applicable to research related to acute myeloid leukemia, small cell lung cancer and neuroendocrine prostate cancer.

Biological activity

In Vitro AUR1545 potently degrades KAT2A/KAT2B and inhibits the growth of NCI-H1048, LASCPC-01 and MOLM-13 cells (1.5 nM, 5 nM, and 1.2 nM, respectively); its DC50 values against KAT2A in the three cell lines are 0.01 nM, 0.67 nM, and 0.11 nM respectively, while its DC50 values against KAT2B are 1.5 nM, 0.16 nM, and 0.075 nM respectively. AUR1545 (0.001-100 nM; 48 h-8 d) induces differentiation in MOLM-13 cells, with an EC50 of 0.3 nM for CD86. AUR1545 (0.01-100 nM; 24 h-7 d) induces epithelial differentiation in LASCPC-01 cells. AUR1545 (0.01-1000 nM; 72 h-21 d) induces microglial differentiation in primary organoids derived from NEPC patients. In Vivo AUR1545 (30 mg/kg; i.p.; once per week) induces 70% tumor growth inhibition and upregulates epithelial differentiation in NCI-H1048 tumor-bearing Nude balb/c mice.

Identifiers

SMILES: O=C1C=2C(CN1C3C(=O)NC(=O)CC3)=CC(=CC2)N4CCN(CC5CCN(C(=O)C6=CC=C(C=C6)[C@H]7C[C@@H](NC8=C(Br)C(=O)N(C)N=C8)CN(C)C7)CC5)CC4
InChIKey: CNPXSLCFWMPKRQ-BFFVTFPMSA-N

Specifications

MW (average): 828.7970
Formula: C₄₁H₅₀BrN₉O₅
CAS No.: 3031593-79-7
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years; In solvent -20°C, 1 month

Solubility

Soluble in DMSO

In vitro: DMSO : 100 mg/mL

Documents

References

[1]. Straley K S, et al. Potent and selective degradation of KAT2A and KAT2B induces profound cell state changes and inhibits growth of AML, SCLC and NEPC model systems[J]. Cancer Research, 2024, 84(6_Supplement): 5795-5795.

Same target

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