PLX647

Modify Date: 2024-01-15 18:49:09

PLX647 structure	Common Name	PLX647
	CAS Number	873786-09-5	Molecular Weight	382.382
	Density	1.4±0.1 g/cm3	Boiling Point	552.8±50.0 °C at 760 mmHg
	Molecular Formula	C₂₁H₁₇F₃N₄	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	288.1±30.1 °C
	Symbol	GHS07	Signal Word	Warning

Use of PLX647

PLX647 is a highly specific dual FMS/KIT kinase inhibitor with IC50 of 28/16 nM respectively.IC50 value: 28/16 nM(FMS/KIT) [1]Target: FMS/KIT dual inhibitorin vitro: PLX647 was tested against a panel of 400 kinases at a concentration of 1 μM, 35-fold above its FMS enzymatic IC50 and 60-fold above its KIT enzymatic IC50. In addition to FMS and KIT, the activities of only nine kinases were inhibited by more than 50%. PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC50 = 0.11 μM) but not OCI-AML5 (IC50 = 1.6 μM), which express wild-type FLT3. PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC50 = 5 μM) [1]. in vivo: PLX647 (40 mg/kg) was dosed orally 4.25 h before LPS injection. Treatment with PLX647 reduced serum TNF-α levels by 85% compared with the vehicle control. In the same experiment, the positive control dexamethasone (0.5 mg/kg, PO) lowered the TNF-α levels by 96%. Treatment with 40 mg/kg PLX647 also resulted in significant inhibition of IL-6 release (75%), with similar potency to dexamethasone (70%) . In the UUO kidneys, treatment with PLX647 [40 mg/kg twice daily (BID)] resulted in reduction in the levels of F4/80+ macrophages by 77% compared with vehicle [1].

Name	2-Pyridinamine, 5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]
Synonym	More Synonyms

Description	PLX647 is a highly specific dual FMS/KIT kinase inhibitor with IC50 of 28/16 nM respectively.IC50 value: 28/16 nM(FMS/KIT) [1]Target: FMS/KIT dual inhibitorin vitro: PLX647 was tested against a panel of 400 kinases at a concentration of 1 μM, 35-fold above its FMS enzymatic IC50 and 60-fold above its KIT enzymatic IC50. In addition to FMS and KIT, the activities of only nine kinases were inhibited by more than 50%. PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC50 = 0.11 μM) but not OCI-AML5 (IC50 = 1.6 μM), which express wild-type FLT3. PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC50 = 5 μM) [1]. in vivo: PLX647 (40 mg/kg) was dosed orally 4.25 h before LPS injection. Treatment with PLX647 reduced serum TNF-α levels by 85% compared with the vehicle control. In the same experiment, the positive control dexamethasone (0.5 mg/kg, PO) lowered the TNF-α levels by 96%. Treatment with 40 mg/kg PLX647 also resulted in significant inhibition of IL-6 release (75%), with similar potency to dexamethasone (70%) . In the UUO kidneys, treatment with PLX647 [40 mg/kg twice daily (BID)] resulted in reduction in the levels of F4/80+ macrophages by 77% compared with vehicle [1].
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Fms Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit Research Areas >> Cancer
References	[1]. Zhang C, et al. Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94. [2]. Louvet C, et al. Tyrosine kinase inhibitors reverse type 1 diabetes in nonobese diabetic mice. Proc Natl Acad Sci U S A. 2008 Dec 2;105(48):18895-900.

Description

Related Catalog

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Fms

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit

Research Areas >> Cancer

References

[1]. Zhang C, et al. Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94.

[2]. Louvet C, et al. Tyrosine kinase inhibitors reverse type 1 diabetes in nonobese diabetic mice. Proc Natl Acad Sci U S A. 2008 Dec 2;105(48):18895-900.

Density	1.4±0.1 g/cm3
Boiling Point	552.8±50.0 °C at 760 mmHg
Molecular Formula	C₂₁H₁₇F₃N₄
Molecular Weight	382.382
Flash Point	288.1±30.1 °C
Exact Mass	382.140533
PSA	53.60000
LogP	4.77
Vapour Pressure	0.0±1.5 mmHg at 25°C
Index of Refraction	1.654
Storage condition	2-8℃

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315-H319-H335
Precautionary Statements	P261-P305 + P351 + P338
RIDADR	NONH for all modes of transport

5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[4-(trifluoromethyl)benzyl]-2-pyridinamine

[5-[(1H-Pyrrolo[2,3-b]pyridin-3-yl)methyl]pyridin-2-yl](4-trifluoromethylbenzyl)amine

2-Pyridinamine, 5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-

PLX 647

PLX647

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: PLX647
Price: Click To Check
Purity: 98.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

DC Chemicals Limited
China
Product Name: PLX647
Price: $500.0/100mg $850.0/250mg $1600.0/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: PLX647
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

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Price: $99/10mM*1mLinDMSO

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PLX647

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