ChemicalBook CAS DataBase List 62004-35-7

62004-35-7

Name	LFM-A13
CAS	62004-35-7
Molecular Formula	C11H8Br2N2O2
MDL Number	MFCD02179204
Molecular Weight	360
MOL File	62004-35-7.mol

Chemical Properties

Boiling point	487.896±45.00 °C(Press: 760.00 Torr)(predicted)
density	1.910±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
storage temp.	−20°C
solubility	DMSO: 15 mg/mL
form	powder
pka	5.202±0.50(predicted)
color	white
InChI	1S/C11H8Br2N2O2/c1-6(16)8(5-14)11(17)15-10-4-7(12)2-3-9(10)13/h2-4,16H,1H3,(H,15,17)
InChIKey	UVSVTDVJQAJIFG-UHFFFAOYSA-N

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302+H312+H332-H315-H319
Precautionary statements	P261-P264-P270-P271-P280-P301+P312+P330-P302+P352+P312+P362+P364-P304+P340+P312-P305+P351+P338+P337+P313-P501
Hazard Codes	Xn
Risk Statements	20/21/22 less more
Safety Statements	36/37 less more
WGK Germany	3
HS Code	2926.90.4801
Storage Class	11 - Combustible Solids

Hazard Information

Uses

LFM-A13 is a novel anti-leukemic agent targeting Bruton''s tyrosine kinase (BTK). LFM-A13 is a BTK inhibitor.

Biological Activity

Potent and selective inhibitor of Bruton's tyrosine kinase (BTK). Inhibits recombinant BTK with an IC 50 value of 2.5 μ M and has no activity on other protein kinases ( including JAK1, JAK3, HCK, EGFR kinase and insulin receptor kinase) at concentrations of up to 278 μ M.

in vivo

LFM-A13 (10 or 50 mg/kg; i.p.) exhibits anti-tumor effects dose dependently in the MMTV/Neu transgenic mouse model of breast cancer^[3]. FM-A13 (50 mg/kg; tiw; i.p.) attenuates DMBA-induced mammary tumorigenesis in mice by modulating a variety of factors associated with cell cycle, survival and apoptosis^[4].

Animal Model:	MMTV/neu transgenic mouse model^[3]
Dosage:	50 or 100 mg/kg
Administration:	Intraperitoneal injection (i.p.); twice a day for 5 consecutive days a week
Result:	Attenuated mammary tumor formation in mice.

Animal Model:	DMBA-induced breast cancer mouse model^[4]
Dosage:	50 mg/kg (or combinated with Paclitaxel (HY-B0015) (10 mg/kg; once per week intraperitoneally))
Administration:	Intraperitoneal injection (i.p.); 3 times a week
Result:	Inhibited DMBA-induced mammary tumor incidence, average tumor number, average tumor weight, and size in BALB/c mice. Significantly decreased PLK1, cyclin D1, CDK-4, P53 and Bcl-2 expression, but increased the expression of p21, IκB, Bax and caspase 3 expression in mice.

IC 50

Plx1: 10 μM (IC₅₀); PLK3: 61 μM (IC₅₀); BRK: 267 μM (IC₅₀); BMX: 281 μM (IC₅₀); FYN: 240 μM (IC₅₀); Met: 215 μM (IC₅₀); Btk: 2.5 μM (IC₅₀)

storage

Store at RT

Supplier

Shanghai Boyle Chemical Co., Ltd.

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Shanghai SuperLan Chemcial Technique Centre

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Aikon International Limited

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Angel Pharmatech, Ltd.

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career henan chemical co

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Energy Chemical

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Jinan Jiuli Biotechnology Co. , Ltd.

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Beijing Jin Ming Biotechnology Co., Ltd.

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Bide Pharmatech Ltd.

Telephone400-1647117 13681763483

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