GW441756(GW-441756)|cas 504433-23-2|DC Chemicals

Cas No.:	504433-23-2
Chemical Name:	(3E)-3-[(1-Methylindol-3-yl)methylidene]-1H-pyrrolo[3,2-b]pyridin-2-one
Synonyms:	1,3-Dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-2H-pyrrolo[3,2-b]pyridin-2-one;GW441756;2H-Pyrrolo[3,2-b]pyridin-2-one, 1,3-dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-;GW 441756,1,3-Dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-2H-pyrrolo[3,2-b]pyridin-2-one;GW 441756,2H-Pyrrolo[3,2-b]pyridin-2-one, 1,3-dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-;GW-441756;(3E)-3-[(1-METHYLINDOL-3-YL)METHYLIDENE]-1H-PYRROLO[3,2-B]PYRIDIN-2-ONE;HMS3677O13;HMS3413O13;ABP000270;SB19388;TZ000920;(E)-3-((1-METHYL-1H-INDOL-3-YL)METHYLENE)-1H-PYRROLO[3,2-B]PYRIDIN-2(3H)-ONE;3-[(E)-(1-Methyl-1H-indole-3-yl)methylene]-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-2-one;GW 441756
SMILES:	O=C1/C(/C2=C(C([H])=C([H])C([H])=N2)N1[H])=C(\[H])/C1=C([H])N(C([H])([H])[H])C2=C([H])C([H])=C([H])C([H])=C12
Formula:	C₁₇H₁₃N₃O
M.Wt:	275.3046
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.IC50 Value: 2 nM [1]Target: TrkAin vitro: GW441756 specifically blocked TrkA-induced cell death in a dose-dependent manner, but there was no effect in uninduced cells. TrkA ability to induce γH2AX production was significantly downregulated by both K-252a and GW441756 in the absence of DNA damage inducer. In addition, it was also suppressed by K-252a during DNA damage by doxorubicin treatment, but not by GW441756 [2].

References:

[1]. Wood ER, Kuyper L, Petrov KG, Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg Med Chem Lett. 2004 Feb 23;14(4):953-7. [2]. Eun Joo Jung, Choong Won Kim, Deok Ryong Kim. Cytosolic accumulation of γH2AX is associated with tropomyosin-related kinase A-induced cell death in U2OS cells. Exp Mol Med. 2008 June 30; 40(3): 276-285.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC11448	LOXO 195(Selitrectinib)	LOXO-195 is a next-generation TRK kinase (TKI) inhibitor, with IC50s of 0.6±0.1 nM, <2.5 nM for TRKA and TRKC respectively.
DC9837	Larotrectinib (LOXO-101 sulfate)	LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
DC7145	GW441756	GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.
DC8300	Entrectinib (RXDX-101)	Entrectinib (RXDX-101), a potent and selective small molecule inhibitor of TrkA/B/C, ROS1, and ALK kinases, has demonstrated early clinical activity when orally administered intermittently under fasting conditions.
DC10448	Belizatinib(TSR-011)	Belizatinib(TSR-011) is an orally available inhibitor of both the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and the tropomyosin-related kinases (TRK) TRKA, TRKB, and TRKC, with potential antineoplastic activity.
DC8029	ANA-12	ANA-12 is a potent and selective TrkB antagonist with anxiolytic and antidepressant activity in mice.