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MRTX-1719

Product Name
MRTX-1719
CAS No.
2630904-45-7
Chemical Name
MRTX-1719
Synonyms
BMS 986504;Navlimetostat;MRTX1719 ，E1024;navlimetostatum;MRTX-1719, 10 mM in DMSO;MRTX-1719,CRC,Histone Methyltransferase,NSCLC,Inhibitor,MTA,MRTX1719,MRTX 1719,inhibit,PRMT5;2-[4-[4-(Aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl]-1-methyl-5-pyrazolyl]-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile;2-(4-(4-(Aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile;(2R)-2-(4-(4-(Aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile;Benzonitrile, 2-[4-[4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl]-1-methyl-1H-pyrazol-5-yl]-4-chloro-6-(cyclopropyloxy)-3-fluoro-, (2R)-
CBNumber
CB29782000
Molecular Formula
C23H18ClFN6O2
Formula Weight
464.89
MOL File
2630904-45-7.mol
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MRTX-1719 Property

Density 
1.58±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
Acetonitrile: Soluble
DMSO: Soluble
pka
11.37±0.40(Predicted)
form 
Solid
color 
White to light yellow
InChIKey
BZKIOORWZAXIBA-UHFFFAOYSA-N
SMILES
CN1N=CC(C2=CC=C3C(NN=C(CN)C3=C2)=O)=C1C1C(=C(Cl)C=C(OC2CC2)C=1C#N)F
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Hazard and Precautionary Statements (GHS)

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MRTX-1719 Chemical Properties,Usage,Production

Uses

Navlimetostat is a potent, orally active, selective PRMT5?MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5?MTA and PRMT5. Navlimetostat 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].

Biological Activity

MRTX-1719 is a potent first-in-class selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAPDEL SDMA cells[1].

in vivo

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

Pharmacokinetic Analysis [2]

ModelRouteDose (mg/kg)Cltotal (mL/min/kg)Vdss (L/kg)t1/2 (h)
CD-1 mouse.i.v.3 836.31.5
Beagle dogi.v.2 143.44.8
Cynomolgus monkeyi.v. 2 152.36.1
ModelRouteDose (mg/kg)Cmax (ug/mL)AUCinf (h*ug/mL)F (%)
CD-1 mouse.p.o.301.164.8580
Beagle dogp.o.10 1.407.4759
Cynomolgus monkeyp.o. 10//41
Animal Model:Lu-99 (an MTAP/CDKN2A-deleted human lung cancer cell line ) xenograft tumor models[2]
Dosage:12.5, 25, 50, and 100 mg/kg/d, 21 day
Administration:Oral gavage
Result:Reduced the tumor volume with 86% tumor growth inhibition (TGI) at 50 mg/kg and 88% TGI at 100 mg/kg.

IC 50

PRMT5

References

[1] Targeting the genetic and immunological drivers of cancer.
[2] CHRISTOPHER R. SMITH*. Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers[J]. Journal of Medicinal Chemistry, 2022, 65 3: 1749-1766. DOI: 10.1021/acs.jmedchem.1c01900

MRTX-1719 Preparation Products And Raw materials

Raw materials

Preparation Products

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MRTX-1719 Suppliers

China 44 United States 3 Global 47
Chengdu DingDang Pharmaceutical Co., Ltd.
Tel
028-86040038 13980902949;
Fax
028-85149890
Email
market@dingdangchem.com
Country
China
ProdList
1853
Advantage
55
Suzhou Meidi Senuo Pharmaceutical Technology Co., Ltd.
Tel
13771642864
Fax
1078336263
Email
snhuyu_2008@126.com
Country
China
ProdList
1165
Advantage
58
Chengdu Junepharma Technology Co., Ltd
Tel
19938173342 19181793067
Email
1486288711@qq.com
Country
China
ProdList
196
Advantage
58
Suzhou Chenrui Biotechnology Co. LTD
Tel
17625585511
Fax
qq：1580084073
Email
1580084073@qq.com
Country
China
ProdList
959
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
15000803246 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
423
Advantage
58
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
15883
Advantage
64
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
Advantage
60
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View Lastest Price from MRTX-1719 manufacturers

Henan Fengda Chemical Co., Ltd
Product
MRTX-1719 2630904-45-7
Price
US $8.00-2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
g-kg-tons, free sample is available
Release date
2024-04-24

2630904-45-7, MRTX-1719Related Search:

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  • Benzonitrile, 2-[4-[4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl]-1-methyl-1H-pyrazol-5-yl]-4-chloro-6-(cyclopropyloxy)-3-fluoro-, (2R)-
  • MRTX-1719,CRC,Histone Methyltransferase,NSCLC,Inhibitor,MTA,MRTX1719,MRTX 1719,inhibit,PRMT5
  • 2-[4-[4-(Aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl]-1-methyl-5-pyrazolyl]-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile
  • (2R)-2-(4-(4-(Aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile
  • MRTX-1719, 10 mM in DMSO
  • Navlimetostat
  • BMS 986504
  • navlimetostatum
  • MRTX1719 ，E1024
  • Benzonitrile, 2-[4-[4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl]-1-methyl-1H-pyrazol-5-yl]-4-chloro-6-(cyclopropyloxy)-3-fluoro-, (2R)- - [AC78275]
  • 2-(4-(4-(Aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile
  • 2630904-45-7
  • C23H18ClFN6O2