2. Epigenetics
  3. Histone Methyltransferase
  4. Navlimetostat hydrochloride

Navlimetostat hydrochloride  (Synonyms: MRTX-1719 hydrochloride; BMS-986504 hydrochloride)

Cat. No.: HY-139611C Purity: 99.61%
COA
SDS
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Navlimetostat hydrochloride is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50s of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat hydrochloride binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study.

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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Navlimetostat hydrochloride:

Navlimetostat hydrochloride Related Antibodies

Top Publications Citing Use of Products
Cell Migration/Invasion Assay
Cell Proliferation/Viability Assay
Bio/Physico-chemical Assay
In Vivo Efficacy Study

    Navlimetostat hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 Dec;13(24):e70526.  [Abstract]

    MRTX1719 (0–10000 nM, 8 days) inhibited the growth of the above five cell types.

    Navlimetostat hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 Dec;13(24):e70526.  [Abstract]

    MRTX1719 (0–10000 nM, 14 days) inhibited the growth of the above four cell types.

    Navlimetostat hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 Dec;13(24):e70526.  [Abstract]

    Following subcutaneous injection of MRTX1719 (10 mg/kg, intraperitoneal injection), the drug concentration in the brain reached its maximum approximately 1 h after administration. The brain-to-plasma concentration ratio of MRTX1719 peaked at 4 h post-administration (brain (A) and serum (B); brain-to-plasma concentration ratio (C)).

    Navlimetostat hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 Dec;13(24):e70526.  [Abstract]

    MRTX1719 (10 mg/kg, intraperitoneal injection) reduced the volume of Hs683-transplanted tumors without reducing the body weight of the mice.

    Navlimetostat hydrochloride purchased from MedChemExpress. Usage Cited in: MedComm (2020). 2024 Sep 20;5(10):e705.  [Abstract]

    Drug dose-response curves for proliferation inhibition and Bliss plots showing the synergistic effects of SCR-7952 in combination with MRTX-1719 on HCT116 MTAP-/- cells over 8 days.

    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

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Navlimetostat hydrochloride is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50s of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat hydrochloride binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study[1][2].

    IC50 & Target[1]

    PRMT5

     

    In Vitro

    Navlimetostat (10 day) hydrochloride inhibits the PRMT5 activity and in MTAP-deleted HCT116 cells not wild type cells, with the IC50 of 8 nM[1]. Navlimetostat (10 day) hydrochloride inhibits the cell viability of MTAP del HCT116 cells with an IC50 value of 12 nM and parental HCT116 cells with an IC50 value of 890 nM[1].

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

    Navlimetostat hydrochloride Related Antibodies
    In Vivo

    Navlimetostat (12.5-100 mg/kg/d for p.o., 21 day) hydrochloride reduces the tumor growth in Lu-99 orthotopic xenograft tumor models[2].

    Pharmacokinetic Analysis [2]

    Model Route Dose (mg/kg) Cltotal (mL/min/kg) Vdss (L/kg) t1/2 (h)
    CD-1 mouse. i.v. 3 83 6.3 1.5
    Beagle dog i.v. 2 14 3.4 4.8
    Cynomolgus monkey i.v. 2 15 2.3 6.1
    Model Route Dose (mg/kg) Cmax (ug/mL) AUCinf (h*ug/mL) F (%)
    CD-1 mouse. p.o. 30 1.16 4.85 80
    Beagle dog p.o. 10 1.40 7.47 59
    Cynomolgus monkey p.o. 10 / / 41

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

    501.34

    Formula

    C23H19Cl2FN6O2
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    [H]Cl.FC1=C(C=C(C(C#N)=[C@]1[C@]2=C(C3=CC=C4C(C(CN)=NNC4=O)=C3)C=NN2C)OC5CC5)Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (199.47 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 1.9947 mL 9.9733 mL 19.9465 mL
    5 mM 0.3989 mL 1.9947 mL 3.9893 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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

    Dosage

    mg/kg

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    (per animal)

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    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.61%

    SDS (252 KB)

    COA (262 KB) HNMR (299 KB) RP-HPLC (265 KB) LCMS (341 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 (sealed storage, away from moisture). 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 1.9947 mL 9.9733 mL 19.9465 mL 49.8664 mL
    5 mM 0.3989 mL 1.9947 mL 3.9893 mL 9.9733 mL
    10 mM 0.1995 mL 0.9973 mL 1.9947 mL 4.9866 mL
    15 mM 0.1330 mL 0.6649 mL 1.3298 mL 3.3244 mL
    20 mM 0.0997 mL 0.4987 mL 0.9973 mL 2.4933 mL
    25 mM 0.0798 mL 0.3989 mL 0.7979 mL 1.9947 mL
    30 mM 0.0665 mL 0.3324 mL 0.6649 mL 1.6622 mL
    40 mM 0.0499 mL 0.2493 mL 0.4987 mL 1.2467 mL
    50 mM 0.0399 mL 0.1995 mL 0.3989 mL 0.9973 mL
    60 mM 0.0332 mL 0.1662 mL 0.3324 mL 0.8311 mL
    80 mM 0.0249 mL 0.1247 mL 0.2493 mL 0.6233 mL
    100 mM 0.0199 mL 0.0997 mL 0.1995 mL 0.4987 mL
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    Navlimetostat hydrochloride 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:

    NavlimetostatMRTX-1719BMS-986504MRTX1719MRTX 1719BMS986504BMS 986504Histone MethyltransferaseInhibitorinhibitorinhibit

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