ML347

Catalog No.S7148

ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM.

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ML347 Chemical Structure

ML347 Chemical Structure
Molecular Weight: 352.39

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM.
Targets ALK2 [1] ALK1 [1] ALK6 [1] ALK3 [1]
IC50 32 nM 46 nM 9.83 μM 10.8 μM
In vitro ML347 also shows potency in BMP-responsive C2C12BRA cells with IC50 of 15 nM, and designated an MLPCN probe. ML347 displays high plasma protein binding in human, rat and mouse plasma. [1]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Kinase assays In brief, compounds are tested at 10 concentrations by threefold serial dilutions starting at 100 mM. In vitro kinase reactions are carried out in the presence of 10 μM (33P)ATP. Eleven human kinases tested are the BMP type-I receptors ALK-1/ACVRL1, ALK2/ACRV1, ALK3/BMPR1A and ALK6/BMPR1B, the TGFb type-I receptors ALK4/ACVR1B and ALK5/TGFbR1, the BMP type-II receptor (BMPR2), the TGFb type-II receptor (TGFbR2), VEGF type-II receptor (KDR/VEGFR2), AMP-activated protein kinase (AMPK-A1/B1/G1) and the human platelet-derived growth factor receptor-β (PDGFRβ).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Engers DW, et al. Bioorg Med Chem Lett. 2013, 23(11), 3248-3252.

Chemical Information

Download ML347 SDF
Molecular Weight (MW) 352.39
Formula

C22 H16 N4

CAS No. 1062368-49-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms LDN-193719
Solubility (25°C) * In vitro DMSO 10 mg/mL (28.37 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Quinoline, 5-[6-(4-methoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]-

Tech Support

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.

Tel: +1-832-582-8158 Ext:3

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