1. Epigenetics
  2. Histone Methyltransferase
  3. PR5-LL-CM01

PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies.

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PR5-LL-CM01

PR5-LL-CM01 화학구조

CAS No. : 1005307-86-7

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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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제품 설명

PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies[1].

IC50 & Target

PRMT5

 

In Vitro

PR5-LL-CM01 has a range of IC50 at 2-4 μM in PDAC cells (PANC1, MiaPaCa2 and AsPC1, and a range of IC50 at 10-11 μM in CRC cells (HT29, HCT116 and DLD1). PR5-LL-CM01 has higher efficacy to specifically inhibit cancer cells and demonstrated low toxicity in normal cells. PR5-LL-CM01 strongly inhibited colony forming ability in both PANC1 and HT29 cells[1].
PR5-LL-CM01 inhibits NF-κB activation and its target gene expression in PDAC and CRC cells[1].
PR5-LL-CM01 (0-15 μM) dramatically decreases TNFα and IL8 expression in both PANC1 and HT29 cells[1].

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

In Vivo

PR5-LL-CM01 (20mg/kg; i.p.; 3 times per week) displays significant anti-tumor effect[1].

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

Animal Model: 6-8 weeks old Male NSG mice (bearing PANC1 or HT29 cells)[1]
Dosage: 20 mg/kg (drug stock dissolved in 1:1 Cremophor:ethanol solution)
Administration: Intraperitoneally 3 times per week; 32 days (PANC1 model); 10 days (HT29 model)
Result: Led to significant tumor inhibition in both PANC1 and HT29 xenografted mice. Did not visibly affect the mice body weight.
분자량

401.51

화학식

C23H27N7

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC=C(NC2=C3C(N(C4=CC=CC=C4)N=C3)=NC(NCCN(C)C)=N2)C=C1C

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

용액&용해도
In Vitro: 

DMSO : 11.11 mg/mL (27.67 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C; 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 2.4906 mL 12.4530 mL 24.9060 mL
5 mM 0.4981 mL 2.4906 mL 4.9812 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 (protect from light). 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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  • 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 Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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.
Calculation results:
Working solution concentration: mg/mL
순도&문서
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 (protect from light). 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 2.4906 mL 12.4530 mL 24.9060 mL 62.2649 mL
5 mM 0.4981 mL 2.4906 mL 4.9812 mL 12.4530 mL
10 mM 0.2491 mL 1.2453 mL 2.4906 mL 6.2265 mL
15 mM 0.1660 mL 0.8302 mL 1.6604 mL 4.1510 mL
20 mM 0.1245 mL 0.6226 mL 1.2453 mL 3.1132 mL
25 mM 0.0996 mL 0.4981 mL 0.9962 mL 2.4906 mL
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  • 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.

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Inquiry Information

상품명:
PR5-LL-CM01
Cat. No.:
HY-109963
수량:
MCE Japan Authorized Agent: