2. Epigenetics
  3. Histone Methyltransferase
  4. Rinzimetostat

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

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Rinzimetostat

Rinzimetostat 화학구조

CAS No. : 2369769-29-7

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 1 publication(s) in Google Scholar

Other Forms of Rinzimetostat:

Rinzimetostat Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Rinzimetostat

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Rinzimetostat (ORIC-944) is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat 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

Rinzimetostat (ORIC-944) (30, 100, 200 mg/kg; op; everyday for 50 days) induces significantly tumor regressions at all dose levels tested[3].
Rinzimetostat (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.
Clinical Trial
분자량

456.51

화학식

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
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
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.

  • 몰농도 계산기

  • 농도 희석 계산기

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.
순도&문서

Purity: 99.90%

SDS (251 KB)

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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Rinzimetostat 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:

Rinzimetostat2369769-29-7ORIC-944ORIC944ORIC 944Histone MethyltransferaseSelectiveorally activeallosteric inhibitorandrogen receptor pathway inhibitorARPImetastatic prostate cancerInhibitorinhibitorinhibit

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상품명:
Rinzimetostat
Cat. No.:
HY-158102
수량:
MCE Japan Authorized Agent:

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SAFETY DATA SHEET (SDS)

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