2. Epigenetics
  3. Histone Acetyltransferase
  4. DS-9300

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.

For research use only. We do not sell to patients.

DS-9300 Chemical Structure

DS-9300 Chemical Structure

CAS No. : 2259641-46-6

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5 mg USD 325 In-stock
10 mg USD 520 In-stock
25 mg USD 1100 Get quote
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Based on 1 publication(s) in Google Scholar

DS-9300 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

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[1].

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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DS-9300 Related Antibodies
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[1].
The pharmacokinetic parameters of DS-9300 in BALB/c mice

PO(10 mg/kg) IV(1 mg/kg)
AUC, AUCu (μM*h) Cmax (μM) T1/2 (h)< Vdss (L/kg) CL, CLu (mL/min/kg) F%
130, 5.33 34 2.4 0.14 1.6, 39 62

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

501.50

Formula

C25H26F3N5O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (249.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9940 mL 9.9701 mL 19.9402 mL
5 mM 0.3988 mL 1.9940 mL 3.9880 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9940 mL 9.9701 mL 19.9402 mL 49.8504 mL
5 mM 0.3988 mL 1.9940 mL 3.9880 mL 9.9701 mL
10 mM 0.1994 mL 0.9970 mL 1.9940 mL 4.9850 mL
15 mM 0.1329 mL 0.6647 mL 1.3293 mL 3.3234 mL
20 mM 0.0997 mL 0.4985 mL 0.9970 mL 2.4925 mL
25 mM 0.0798 mL 0.3988 mL 0.7976 mL 1.9940 mL
30 mM 0.0665 mL 0.3323 mL 0.6647 mL 1.6617 mL
40 mM 0.0499 mL 0.2493 mL 0.4985 mL 1.2463 mL
50 mM 0.0399 mL 0.1994 mL 0.3988 mL 0.9970 mL
60 mM 0.0332 mL 0.1662 mL 0.3323 mL 0.8308 mL
80 mM 0.0249 mL 0.1246 mL 0.2493 mL 0.6231 mL
100 mM 0.0199 mL 0.0997 mL 0.1994 mL 0.4985 mL
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DS-9300 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DS-93002259641-46-6DS9300DS 9300Histone AcetyltransferaseHATsHATEP300/CBPanticancerprostate cancerInhibitorinhibitorinhibit

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