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LY364947

Cat. No. M2016
LY364947 Structure
Synonym:

HTS 466284

Size Price Availability Quantity
10mg USD 95 In stock
50mg USD 320 In stock
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Biological Activity

LY-364947 is a selective, ATP-competitive inhibitor of Transforming Growth Factor-β Type I receptor kinase. LY364947 inhibits TGF-β-dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3) (IC50 values are 47 and 89 nM respectively). LY364947 is much less potent at related kinases, with IC50 of 400 nM for TGF-β RII and IC50 of 1400 nM for mixed lineage kinase-7 (MLK-7), a kinase in the MAP kinase signal pathway and closely related to TGF-β RII. LY364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. LY364947 (25 mg/kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 272.31
Formula C17H12N4
CAS Number 396129-53-6
Purity 99.47%
Solubility DMSO
Storage at -20°C
References

TGFβ1 inhibition increases the radiosensitivity of breast cancer cells in vitro and promotes tumor control by radiation in vivo.
Bouquet F, et al. Clin Cancer Res. 2011 Nov 1;17(21):6754-65. PMID: 22028490.

The specificities of small molecule inhibitors of the TGFß and BMP pathways.
Vogt J, et al. Cell Signal. 2011 Nov;23(11):1831-42. PMID: 21740966.

Smad4 regulates claudin-1 expression in a transforming growth factor-beta-independent manner in colon cancer cells.
Shiou SR, et al. Cancer Res. 2007 Feb 15;67(4):1571-9. PMID: 17308096.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY364947, HTS 466284 supplier, TGF-beta, inhibitors

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