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GGTI-2154 hydrochloride 

Cat. No.: HY-16229A
Handling Instructions

GGTI-2154 hydrochloride is a potent and selective inhibitor geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 hydrochloride shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 hydrochloride can be used for the research of cancer.

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

GGTI-2154 hydrochloride Chemical Structure

GGTI-2154 hydrochloride Chemical Structure

CAS No. : 478908-50-8

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Description

GGTI-2154 hydrochloride is a potent and selective inhibitor geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 hydrochloride shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 hydrochloride can be used for the research of cancer[1][2].

IC50 & Target

IC50: 21 nM (GGTase I)[1]

In Vitro

GGTI-2154 inhibits the transfer of geranylgeranyl from [3H]GGPP to H-Ras CVLL, with an IC50 of 21 nM[1].

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

In Vivo

GGTI-2154 (100 mg/kg/day; s.c. for 14 days) induces breast tumor regression in MMTV-ν-Ha-Ras transgenic mice[2].
GGTI-2154 (50 mg/kg/day; i.p. for 50 day) inhibits A-549 tumor growth in nude mice by 60%[1].

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

Animal Model: MMTV-v-Ha-ras transgenic mice bearing mammary carcinoma[2]
Dosage: 100 mg/kg/day
Administration: S.c. with osmotic mini-pumps for 14 days
Result: Halted the tumors aggressive growth.
Resulted in rapid tumor regression within 3 days of initiation of drug treatment.
Molecular Weight

456.97

Formula

C₂₄H₂₉ClN₄O₃

CAS No.
SMILES

CC(C)C[[email protected]@H](C(O)=O)NC(C1=CC=C(NCC2=CN=CN2)C=C1C3=CC=CC=C3C)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

GGTI-2154GGTI2154GGTI 2154OthersgeranylgeranyltransferaseIGGTasecancerInhibitorinhibitorinhibit

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GGTI-2154 hydrochloride
Cat. No.:
HY-16229A
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