CGP 57380

Modify Date: 2024-01-02 20:36:00

CGP 57380 structure	Common Name	CGP 57380
	CAS Number	522629-08-9	Molecular Weight	244.228
	Density	1.6±0.1 g/cm3	Boiling Point	541.6±50.0 °C at 760 mmHg
	Molecular Formula	C₁₁H₉FN₆	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	281.4±30.1 °C
	Symbol	GHS07	Signal Word	Warning

Use of CGP 57380

CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.

Name	3-N-(4-fluorophenyl)-2H-pyrazolo[3,4-d]pyrimidine-3,4-diamine
Synonym	More Synonyms

Description	CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
Related Catalog	Signaling Pathways >> MAPK/ERK Pathway >> MNK Research Areas >> Cancer
Target	MNK1:2.2 μM (IC50)
In Vitro	CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC50 of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells[1]. CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy[2]. CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs)[3]. CGP57380 prevents the serial replating function of BC progenitors[4].
In Vivo	CGP57380 (40 mg/kg/d i.p.) potently extinguishes the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs[4].
Kinase Assay	Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/mL), Mkk6(E) (30 ng/mL), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/mL), HA-eIF4E (10 ng/mL), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03-3 ng/mL) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors.
Animal Admin	CD34+ cells (5×105) or GMPs (1×105) are resuspended in 25 μL 1% FBS/PBS solution and injected into the right femur of 8- to 10-wk-old sublethally irradiated (200 cGy) female mice (n=5 mice per group). Mice injected with 1% FBS/PBS solution serve as a sham control for each experiment. Beginning at 4 wk posttransplantation, mice are monitored for engraftment of human cells by flow cytometry. At 6 wk after transplantation, engrafted mice are treated with vehicle alone, dasatinib (5 mg/kg/d) by gavage, or CGP57380 (40 mg/kg/d) intraperitoneally for 3 wk (n=5 mice per group). At the end of treatment, mice are euthanized, and CD45+ cells are isolated from BM and spleen by using anti-human CD45-specific immunomagnetic microbeads. An aliquot of 1×105 human CD45+ cells is seeded into methylcellulose for the colony forming cell (CFC) assay, and colonies are enumerated after 2 wk. All of the remaining human cells from each primary transplant recipient are then transplanted by intrafemoral injection into secondary recipients, and human engraftment is monitored at 2-wk intervals beginning at 4 wk. At the end of 16 wk, all mice are euthanized. Engraftment in BM and blood is assessed by flow cytometry, and BCR-ABL1 transcripts are detected by RT-PCR.
References	[1]. Knauf U, et al. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol. 2001 Aug;21(16):5500-11. [2]. Ishida M, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res. 2003 Dec 12;93(12):1218-24. Epub 2003 Nov 6 [3]. Chrestensen CA, et al. Loss of MNK function sensitizes fibroblasts to serum-withdrawal induced apoptosis. Genes Cells. 2007 Oct;12(10):1133-40. [4]. Lim S, et al. Targeting of the MNK-eIF4E axis in blast crisis chronic myeloid leukemia inhibits leukemia stem cell function. Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):E2298-307

Density	1.6±0.1 g/cm3
Boiling Point	541.6±50.0 °C at 760 mmHg
Molecular Formula	C₁₁H₉FN₆
Molecular Weight	244.228
Flash Point	281.4±30.1 °C
Exact Mass	244.087280
PSA	92.51000
LogP	1.28
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.809
Storage condition	-20℃

CGP 57380 MSDS(Chinese)

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H319
Precautionary Statements	P305 + P351 + P338
Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR	NONH for all modes of transport

Targeting RNA transcription and translation in ovarian cancer cells with pharmacological inhibitor CDKI-73.

Oncotarget 5(17) , 7691-704, (2014)

Dysregulation of cellular transcription and translation is a fundamental hallmark of cancer. As CDK9 and Mnks play pivotal roles in the regulation of RNA transcription and protein synthesis, respectiv...

MNKs act as a regulatory switch for eIF4E1 and eIF4E3 driven mRNA translation in DLBCL.

Nat. Commun. 5 , 5413, (2014)

The phosphorylation of eIF4E1 at serine 209 by MNK1 or MNK2 has been shown to initiate oncogenic mRNA translation, a process that favours cancer development and maintenance. Here, we interrogate the M...

Pharmacologic co-inhibition of Mnks and mTORC1 synergistically suppresses proliferation and perturbs cell cycle progression in blast crisis-chronic myeloid leukemia cells.

Cancer Lett. 357(2) , 612-23, (2015)

The Ras/Raf/MAPK and PI3K/Akt/mTORC1 cascades are two most aberrantly regulated pathways in cancers. As MAPK-interacting kinases (Mnks) are part of the convergent node of these two pathways, and play ...

1H-Pyrazolo[3,4-d]pyrimidine-3,4-diamine, N-(4-fluorophenyl)-

N-(4-Fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidine-3,4-diamine

CGP57380 N3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidine-3,4-diamine

CGP-57380

CGP 57380

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: CGP-57380
Price: Negotiable
Purity: 98.0%
Delivery: 10 Day
Contact: Huang
Email: sales@echemcloud.com

DC Chemicals Limited
China
Product Name: CGP-57380
Price: $450.0/100mg $900.0/250mg $1800.0/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: CGP-57380
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

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Price: $196/10mM*1mLinDMSO

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CGP 57380

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