DS-9300 free base · Synonyms: DS 9300 · DS9300
DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor.
For research use only. Not for human or veterinary use.
DS-9300 structure
CAS No.: 2259641-46-6
Pack sizes & pricing
Description
DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research .
Biological activity
In Vitro DS-9300 inhibits the growth of prostate cancer cell lines with the IC50 values of 0.6, 6.5, 3.4 and 287.2 nM for VCaP, 22Rv1, LNCaP and PC3 cells, respectively, indicating that it could effectively inhibit the growth of prostate cancer cell lines by inhibiting histone acetylation and down-regulating PSA expression In Vivo DS-9300 (p.o., 0.3-3 mg/kg, once daily, 33days) shows dose-dependent antitumor activity with 39%, 74% and 109% tumor growth inhibition at 0.3, 1 and 3 mg/kg, respectively, and no significant toxic effects in Castrated VCaP xenograft mouse model
Identifiers
- SMILES
-
COC1=CC=C(C=C1)C2(CCC(F)(CC2)F)C(N3C[C@@H](C[C@@H]3C(NC4=NC5=C(NN=C5)C=C4)=O)F)=O - InChIKey
-
UCKDTCZSOLMOMQ-OXQOHEQNSA-N
Specifications
- MW (average)
- 501.5008
- Formula
- C25H26F3N5O3
- CAS No.
- 2259641-46-6
- Physical state
- Solid
- Color
- White to off-white
- 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 ; In solvent -20°C, 1 month
Solubility
Soluble in DMSO
- In vitro
- DMSO : 100 mg/mL
Documents
References
Same target
Search Histone AcetyltransferaseSame research area
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