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  4. ORIC-944

ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.

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

ORIC-944 Chemical Structure

ORIC-944 Chemical Structure

CAS No. : 2369769-29-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 427 In-stock
Solution
10 mM * 1 mL in DMSO USD 427 In-stock
Solid
1 mg USD 170 In-stock
5 mg USD 425 In-stock
10 mg USD 680 In-stock
25 mg USD 1365 In-stock
50 mg USD 2185 In-stock
100 mg USD 3500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of ORIC-944:

ORIC-944 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.

IC50 & Target

polycomb repressive complex 2; PRC2[1]
In Vivo

ORIC-944 (30, 100, 200 mg/kg; op; everyday for 50 days) induces significantly tumor regressions at all dose levels tested[3].
ORIC-944 (30 mg/kg; op; everyday for 30 days) demonstrates strong single agent activity to enzalutamide in prostate cancer xenograft model[3].

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

Animal Model: KARPAS-422 DLBCL xenograft model[1]
Dosage: 30, 100, 200 mg/kg
Administration: Oral gavage (p.o.)
Result: Had well tolerated at all dose levels assessed compared to tazemetostat at a clinically relevant dose.
Animal Model: 22Rv1 model
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.)
Result: Made average tumor volume ± SEM, with n=8-10/group.
Had a significant difference in ORIC-944 treatment group vs vehicle.
Molecular Weight

456.51

Formula

C26H25FN6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C=CC(CN(C)C)=C1)C2=CN=C(N3C=C(N=C23)C#N)NCC4=C(C=CC5=C4CCO5)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (219.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1905 mL 10.9527 mL 21.9053 mL
5 mM 0.4381 mL 2.1905 mL 4.3811 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.90%

COA (249 KB) HNMR (137 KB) RP-HPLC (137 KB) LCMS (107 KB)

Handling Instructions (2659 KB)
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 2.1905 mL 10.9527 mL 21.9053 mL 54.7633 mL
5 mM 0.4381 mL 2.1905 mL 4.3811 mL 10.9527 mL
10 mM 0.2191 mL 1.0953 mL 2.1905 mL 5.4763 mL
15 mM 0.1460 mL 0.7302 mL 1.4604 mL 3.6509 mL
20 mM 0.1095 mL 0.5476 mL 1.0953 mL 2.7382 mL
25 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1905 mL
30 mM 0.0730 mL 0.3651 mL 0.7302 mL 1.8254 mL
40 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3691 mL
50 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 mL
60 mM 0.0365 mL 0.1825 mL 0.3651 mL 0.9127 mL
80 mM 0.0274 mL 0.1369 mL 0.2738 mL 0.6845 mL
100 mM 0.0219 mL 0.1095 mL 0.2191 mL 0.5476 mL
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ORIC-944 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:

ORIC-9442369769-29-7ORIC944ORIC 944OthersSelectiveorally activeallosteric inhibitorandrogen receptor pathway inhibitorARPImetastatic prostate cancerInhibitorinhibitorinhibit

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