Cyt387

Validation & Quality Control

Product Citations(1)

Blood, 2012, 120(19), 4093-4103

Quality Control & MSDS

Related Compound Libraries

Cyt387 is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) Inhibitor Library (96-well) Kinase Inhibitor Library (96-well) Tyrosine Kinase Inhibitor Library (96-Well)

Product Information

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Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1378	Ruxolitinib (INCB018424)	<1 mg/mL	61 mg/mL	61 mg/mL
S5001	Tofacitinib citrate (CP-690550 citrate)	<1 mg/mL	101 mg/mL	<1 mg/mL
S2736	TG101348 (SAR302503)	<1 mg/mL	105 mg/mL	21 mg/mL
S2789	Tofacitinib (CP-690550, Tasocitinib)	<1 mg/mL	63 mg/mL	<1 mg/mL
S2162	AZD1480	<1 mg/mL	70 mg/mL	5 mg/mL
S1143	AG-490	<1 mg/mL	59 mg/mL	6 mg/mL
S2219	Cyt387	<1 mg/mL	83 mg/mL	<1 mg/mL
S2686	NVP-BSK805	3 mg/mL	113 mg/mL	15 mg/mL
S2692	TG101209	<1 mg/mL	102 mg/mL	<1 mg/mL
S2851	Baricitinib (LY3009104, INCB28050)	<1 mg/mL	74 mg/mL	<1 mg/mL
S2796	WP1066	<1 mg/mL	72 mg/mL	<1 mg/mL
S1134	AT9283	<1 mg/mL	76 mg/mL	38 mg/mL
S2806	CEP33779	<1 mg/mL	93 mg/mL	<1 mg/mL
S2214	AZ 960	<1 mg/mL	71 mg/mL	3 mg/mL
S2867	WHI-P154	<1 mg/mL	75 mg/mL	<1 mg/mL
S2179	LY2784544	<1 mg/mL	94 mg/mL	9 mg/mL
S2902	S-Ruxolitinib	5 mg/mL	61 mg/mL	61 mg/mL
S8004	ZM 39923 HCl	<1 mg/mL	30 mg/mL	8 mg/mL

Product Description

Biological Activity Protocol Chemical Information Product Citations Tech Support & FAQs

Biological Activity

Description	CYT387 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50 of 11 nM and 18 nM, respectively.
Targets	JAK1	JAK2	JAK3
IC50	11 nM	18 nM	155 nM ^[1]
In vitro	CYT387 inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, CYT387 also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC50 of 200 nM, 1 nM and 700 nM, respectively. In addition, CYT387 has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2μ-4 μM. ^[1] A recent study shows that CYT387 inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, CYT387 induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) cells. ^[2]
In vivo	In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines. ^[3]
Clinical Trials	Cyt387 is currently in Phase I/II clinical trials in patients with primary myelofibrosis or post-polycythemia vera or post-essential thrombocythemia myelofibrosis.
Features

Protocol(Only for Reference)

Kinase Assay: ^[1]

Cell-free kinase activity assays	Glutathione-S-transferase (GST)-tagged JAK kinase domains expressed in insect cells are purified before use in a peptide substrate phosphorylation assay. Assays are carried out in 384-well optiplates using an Alphascreen Protein Tyrosine Kinase P100 detection kit and a PerkinElmer Fusion Alpha instrument.

Cell Assay: ^[1]

Cell lines	Ba/F3, Ba/F3-JAK2V617F and Ba/F3-MPLW515L cells
Concentrations	0 to 10 μM
Incubation Time	72 hours
Method	Ba/F3 cells expressing JAK2V617F (Ba/F3-JAK2V617F) and MPLW515L (Ba/F3-MPLW515L) mutants, as well as CHRF-288-11 (JAK2T875N) and CMK (JAK3A572V) cells are used. The TEL/JAK2 and TEL/JAK3 fusions are generated and introduced into Ba/F3 murine cells. The TEL/JAK2- or TEL/JAK3-transfected cells are cultured in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal calf serum (FCS). Ba/F3 wild-type cells are cultured in RPMI containing 10% FCS supplemented with 5 ng/mL murine IL-3. Proliferation is measured using the Alamar Blue assay after incubating for 72 hours at 37 °C with 5% CO₂.

Animal Study: ^[3]

Animal Models	Balb/c mice are transplanted with bone marrow transduced with a JAK2V617F retrovirus.
Formulation	CYT387 is dissolved in NMP (120 mg/mL final; 1-methyl-2-pyrrolidinone, Chromasolv Plus). Subsequently, the CYT387/NMP mix is diluted with 0.14 M Captisol to a concentration of 6 mg/mL and further diluted with 0.1M Captisol to a final concentration of 4 mg/mL.
Dosages	≤50 mg/kg
Administration	Administered via p.o.

1

References

Chemical Information

Download Cyt387 SDF

Molecular Weight (MW)	414.46
Formula	C₂₃H₂₂N₆O₂
CAS No.	1056634-68-4, 1056636-08-8 (XHCl)
Synonyms	CYT 11387

Solubility (25°C) DMSO 83 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide

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Research Area

Product Citations (1)

IFNγR signaling mediates alloreactive T cell trafficking and GvHD. [Choi J, et al. Blood 2012;120(19), 4093-4103]
PubMed: 22972985

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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AT9283 is a potent pan-Aurora inhibitor for Aurora A, Aurora B, JAK3, JAK2 and Abl with IC50 of 3 nM, 3 nM, 1.1 nM, 1.2 nM and 4 nM, respectively.
AG-490
AG-490 (Tyrphostin B42) is an inhibitor of EGFR, ErbB2 and JAK2 with IC50 of 0.1 μM, 13.5 μM, and ~10 μM, respectively.
AZD1480

AZD1480 is a novel ATP-competitive inhibitor of JAK1 and JAK2 with IC50 of 1.3 nM and 0.26 nM, respectively.
LY2784544

LY2784544 is selective to V617F mutant JAK2 with IC50 of 55 nM in Ba/F3 cells.
AZ 960

AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and K_i of <3 nM and 0.45 nM, respectively.
NVP-BSK805

NVP-BSK805 is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM.
TG101209

TG101209 is a potent inhibitor of JAK2, Flt3 and RET with IC50 of 6 nM, 25 nM and 17 nM, respectively.
TG101348 (SAR302503)

TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM.
Tofacitinib (CP-690550, Tasocitinib)

CP-690550 is a novel inhibitor of JAK3 with IC50 of 1 nM.
WP1066
WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells .

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Validation & Quality Control

Product Citations(1)

Quality Control & MSDS

Related Compound Libraries

Cyt387 is available in the following compound libraries:

Product Information

Compare JAK Inhibitors

Research Area

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: ^[1]

Cell Assay: ^[1]

Animal Study: ^[3]

References

Chemical Information

Research Area

Product Citations (1)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related JAK Inhibitors

JAK/STAT Pathway Products

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Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S1378	Ruxolitinib (INCB018424)	<1 mg/mL	61 mg/mL	61 mg/mL
S5001	Tofacitinib citrate (CP-690550 citrate)	<1 mg/mL	101 mg/mL	<1 mg/mL
S2736	TG101348 (SAR302503)	<1 mg/mL	105 mg/mL	21 mg/mL
S2789	Tofacitinib (CP-690550, Tasocitinib)	<1 mg/mL	63 mg/mL	<1 mg/mL
S2162	AZD1480	<1 mg/mL	70 mg/mL	5 mg/mL
S1143	AG-490	<1 mg/mL	59 mg/mL	6 mg/mL
S2219	Cyt387	<1 mg/mL	83 mg/mL	<1 mg/mL
S2686	NVP-BSK805	3 mg/mL	113 mg/mL	15 mg/mL
S2692	TG101209	<1 mg/mL	102 mg/mL	<1 mg/mL
S2851	Baricitinib (LY3009104, INCB28050)	<1 mg/mL	74 mg/mL	<1 mg/mL
S2796	WP1066	<1 mg/mL	72 mg/mL	<1 mg/mL
S1134	AT9283	<1 mg/mL	76 mg/mL	38 mg/mL
S2806	CEP33779	<1 mg/mL	93 mg/mL	<1 mg/mL
S2214	AZ 960	<1 mg/mL	71 mg/mL	3 mg/mL
S2867	WHI-P154	<1 mg/mL	75 mg/mL	<1 mg/mL
S2179	LY2784544	<1 mg/mL	94 mg/mL	9 mg/mL
S2902	S-Ruxolitinib	5 mg/mL	61 mg/mL	61 mg/mL
S8004	ZM 39923 HCl	<1 mg/mL	30 mg/mL	8 mg/mL

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Cyt387

Validation & Quality Control

Product Citations(1)

Quality Control & MSDS

Related Compound Libraries

Cyt387 is available in the following compound libraries:

Product Information

Compare JAK Inhibitors

Research Area

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: [1]

Cell Assay: [1]

Animal Study: [3]

References

Chemical Information

Research Area

Product Citations (1)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related JAK Inhibitors

JAK/STAT Pathway Products

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Kinase Assay: ^[1]

Cell Assay: ^[1]

Animal Study: ^[3]