ZINC69391|CAS 303094-67-9|DC Chemicals

Cas No.:	303094-67-9
Chemical Name:	2-(4,6-Dimethylpyrimidin-2-yl)-1-[2-(trifluoromethyl)phenyl]guanidine
Synonyms:	2-(4,6-dimethylpyrimidin-2-yl)-1-[2-(trifluoromethyl)phenyl]guanidine;N'-(4,6-dimethylpyrimidin-2-yl)-N-[2-(trifluoromethyl)phenyl]guanidine;N-(4,6-Dimethyl-2-pyrimidinyl)-N'-[2-(trifluoromethyl)phenyl]-guanidine;SMSF0013930;CB12619;Z56785930
SMILES:	FC(C1=C([H])C([H])=C([H])C([H])=C1N([H])C(N([H])[H])=NC1=NC(C([H])([H])[H])=C([H])C(C([H])([H])[H])=N1)(F)F
Formula:	C₁₄H₁₄F₃N₅
M.Wt:	309.2897
Purity:	>98%
Sotrage:	0°C (short term), -20°C (long term), desiccated

Description:	Novel specific Rac1 inhibitor, interferring with the interaction of Rac1 with Dock180, a relevant Rac1 activator in glioma invasion, and to reduce Rac1-GTP levels
In Vivo:	ZINC69391 (25 mg/kg; i.p; daily for 21 days) impairs metastatic lung colonization in a syngeneic animal model[3]. Animal Model: Specific pathogen-free female BALB/c inbred mice (bearing F3II cells)[3] Dosage: 25 mg/kg body weight Administration: I.p; daily for 21 days Result: Significantly reduced by about 60% the formation of total metastatic lung colonies.
In Vitro:	ZINC69391 inhibits growth of U937, HL-60, KG1A and Jurkat cells with IC50s ranging from 41 to 54 μM[1]. ZINC69391 (50-100 μM; 24 hours) augments the enzymatic activity of caspase 3 in a concentration dependent manner[1]. ZINC69391 (0-125 μM; 72h) reduces cell proliferation of human glioma cells[2]. ZINC69391 (50-100 μM; 48 hours) triggers cell cycle arrest[2]. ZINC69391 (50 μM; 24 hours) triggers apoptosis on human acute leukemic cells[1]. Cell Proliferation Assay[2] Cell Line: U-87 MG, LN229 cells Concentration: 0-125μM Incubation Time: 72 hours Result: Reduced cell proliferation in a concentration-dependent manner. Cell Cycle Analysis[2] Cell Line: LN229 cells Concentration: 50, 100 μM Incubation Time: 48 hours Result: Resulted in a significant increased percentage of cells in the sub-G0/G1 phase in a concentration dependent manner. Apoptosis Analysis[1] Cell Line: HL-60, U937 and KG1A cell lines Concentration: 50 μM Incubation Time: 24 hours Result: Led to a significant increase in apoptotic cells.
References:	[1]. Cabrera M, et al. Pharmacological Rac1 inhibitors with selective apoptotic activity in human acute leukemic cell lines. Oncotarget. 2017;8(58):98509‐98523. Published 2017 Oct 4. [2]. Cardama GA, et al. Proapoptotic and antiinvasive activity of Rac1 small molecule inhibitors on malignant glioma cells. Onco Targets Ther. 2014;7:2021‐2033. Published 2014 Oct 30. [3]. Cardama GA, et al. Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines. Anticancer Agents Med Chem. 2014;14(6):840‐851.

Cat. No.	Product name	Field of application
DC31074	Isopropyl myristate	Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC75868	AZ14133346	AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75865	TI17	TI17 represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.
DC75816	Nisoxetine	Nisoxetine acts as a highly selective and potent noradrenaline transporter (NET) antagonist, exhibiting a binding affinity (Kd) of 0.76 nM. In addition to its antidepressant properties, nisoxetine functions as a local anesthetic by inhibiting voltage-gated sodium channels. This dual pharmacological activity makes it a compound of interest for both neurological and pain management research.
DC75641	GENZ-644282 TFA salt	Genz-644282, also known as SAR402674, is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations.
DC75325	PSMA-617 TFA	PSMA-617, also know as vipivotide tetraxetan, is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer. PSMA617 possesses a small peptide, which was designed to target prostate-specific membrane antigen (PSMA). PSMA617 demonstrates high radiolytic stability for at least 72 h. PSMA617 has high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined). 177 Lu-PSMA-617 offers a potential additional life-prolonging treatment option for men with mCRPC.
DC75202	Fosaprepitant free acid	Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4
DC74748	O4I4	O4I4 (compound 23) is a OCT4-inducing compound with metabolical stability.
DC74684	ZH8667	ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist.
DC74646	EB-PSMA-617	EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer.