2396465-33-9

Name	Cyclopentanecarboxamide, 3-[[3-bromo-1-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N,1-dimethyl-, (1R,3R)-
CAS	2396465-33-9
Molecular Formula	C22H23BrN8OS
Molecular Weight	527.44
MOL File	2396465-33-9.mol

Synonyms

GCN2-IN-7 Cyclopentanecarboxamide, 3-[[3-bromo-1-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N,1-dimethyl-, (1R,3R)-

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Chemical Properties

density	1.67±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
form	Solid
pka	16.40±0.40(Predicted)
color	White to off-white

Hazard Information

Uses

GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo[1].

in vivo

GCN2-IN-7 (oral gavage; 15 mg/kg; BID; 17 d) shows robust target engagement in vivo at a reasonable dose^[1].
GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) inhibits tumor growth in vivo of the LL2 syngeneic mouse tumor model^[1].

Animal Model:	Balb/c mice injected with RENCA cells^[1]
Dosage:	15 mg/kg
Administration:	Oral gavage; 15 mg/kg; BID; 17 days
Result:	Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues. Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group.

Animal Model:	LL2 syngeneic mouse model^[1]
Dosage:	50 mg/kg
Administration:	Oral gavage; 50 mg/kg; BID; 17 days
Result:	Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.

storage

Store at -20°C

References

[1] Jackson JJ, et al. Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy. J Med Chem. 2022 Sep 20. DOI:10.1021/acs.jmedchem.2c00736

Spectrum Detail

Cyclopentanecarboxamide, 3-[[3-bromo-1-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N,1-dimethyl-, (1R,3R)-(2396465-33-9)¹HNMR

Supplier

Shanghai Pengque Chemical Technology Co., LTD

Telephone15317013857 15901926503

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList1022031/0_EN.htm

Nantong Hi-Future Biotechnology Co., Ltd

Telephone+86-0513; 18051384581

Websitehttps://www.chemhifuture.com/

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Jiangsu Aikon Biopharmaceutical R&D Co.,Ltd.

Telephone025-66061636 19370895928

Websitehttps://www.aikonchem.com/

Shanghai Amole Biotechnology Co., Ltd.

Telephone13370042665 18916960931

Websitehttps://www.amole.com.cn/

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