ChemicalBook CAS DataBase List 2629314-68-5

2629314-68-5

Name	INDEX NAME NOT YET ASSIGNED
CAS	2629314-68-5
Molecular Formula	C24H17FN6O
MDL Number	MFCD34473210
Molecular Weight	424.43
MOL File	2629314-68-5.mol

Chemical Properties

density	1.44±0.1 g/cm3(Predicted)
storage temp.	-20°C, protect from light
solubility	DMSO : 30 mg/mL (70.68 mM; ultrasonic and warming and heat to 60°C)
form	Solid
pka	11.36±0.40(Predicted)
color	White to light brown
InChI	InChI=1S/C24H17FN6O/c1-31-23(22-18(10-26)15-5-3-2-4-13(15)9-20(22)25)19(12-28-31)14-6-7-16-17(8-14)21(11-27)29-30-24(16)32/h2-9,12H,11,27H2,1H3,(H,30,32)
InChIKey	BPTYWAYMKBEXES-UHFFFAOYSA-N
SMILES	C1(C#N)=C2C(C=CC=C2)=CC(F)=C1C1N(C)N=CC=1C1C=CC2=C(C=1)C(CN)=NNC2=O

Hazard Information

Uses

MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor[1].

Biological Activity

MRTX9768 is a potent, orally active PRMT5 inhibitor. MRTX9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors[1]. MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1]. In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors[1].

in vivo

In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow^[1].
MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors (such as glioblastoma)^[1]^[2].
MRTX9768 (PO dose 30 mg/kg in CD-1 mouse and beagle dog, 10 mg/kg in cynomolgus monkey) has a favorable ADME profile (>50% bioavailability in mice and dogs, moderate to high clearance, No changes in RBC parameters when administered well above efficacious concentrations (1000 mg/kg))^[3].
MRTX9768 (100 mg/kg, orally, BID, 6/21 days) results in SDMA inhibition maintaining 3 days after dosing is stopped^[3].

IC 50

PRMT5

storage

-20°C, protect from light

References

[1]. Christopher R. et al. Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2021; 2021 Apr 10-15 and May 17-21. Philadelphia (PA): AACR; Cancer Res 2021;81(13_Suppl):Abstract nr LB003.

Spectrum Detail

Supplier

ShangHai Caerulum Pharma Discovery Co., Ltd.

Telephone18149758185 18149758185

Websitehttp://www.caerulumpharma.com

Shanghai Chaolan Chemical Technology Center

TelephoneQQ：65489617 13301690235

Websitehttp://www.atkchemical.com/

Suzhou Chenrui Biotechnology Co. LTD

Telephone 17625585511

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList660257/0_EN.htm

Nantong Hi-Future Biotechnology Co., Ltd

Telephone+86-0513; 18051384581

Websitehttps://www.chemhifuture.com/

Bide Pharmatech Ltd.

Telephone400-1647117 13681763483

Websitehttps://www.bidepharm.com/

TargetMol Chemicals Inc.

Telephone4008200310 15002144251

Websitehttps://www.targetmol.cn/

ShangHai Caerulum Pharma Discovery Co., Ltd.

Telephone15000803246 18149758185

Websitehttp://www.caerulumpharma.com/

Shanghai Tachizaki Biomedical Research Center

Telephone 18014399201

Websitehttp://www.chemlab-tachizaki.com/

Wuhan Jingkangen Biomedical Technology Co., Ltd

Telephone13720134139 086-15871494362 13720134139

Websitehttps://www.jknbiochem.com

Nantong QuanYi Biotechnology Co., Ltd

Telephone0513-66337626 18051384581

Websitehttps://www.chemhifuture.com/

Shanghai Yifei Biotechnology Co. , Ltd.

Telephone021-65675885 18964387627

Websitehttp://www.efebio.com

Beijing Boorsen Biotechnology Co., Ltd

Telephone400-901-9800 18611424007

Websitehttp://www.bioss.com.cn/

Nanjing Shizhou Biology Technology Co.,Ltd

Telephone025-85560043 15850508050

Websitehttp://www.synzest.com

Changsha Fuzhen Biotechnology Co.，LTD

Telephone15111215862 18229892877

Websitehttp://www.fuzhenbiochem.com/

RD International Technology Co., Limited

Telephone 18024082417

Websitehttps://www.ruidiresearch.com

Olix ( Hubei) Pharmaceutical Technology Co., Ltd

Telephone17316404525 17316404525

Websitehttps://www.olix.cn

ATK CHEMICAL COMPANY LIMITED

Telephone+undefined-21-51877795

Websitehttp://www.atkchemical.com

NANJING YINGWEN BIOTECHNOLOGY CO LTD

Telephone +8613382787392

Websitehttps://www.aeechem.com/

1of4

Related Products

Send Inquriy