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HG-7-85-01

Name: HG-7-85-01
Brand: TargetMol
SKU: T38653
Price: 68 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T38653Cas No. 1258391-13-7

HG-7-85-01 is a novel ATP-competitive and type II tyrosine kinase inhibitor targeting both wild-type and watchman mutant BCR-ABL, PDGFRα, Kit, and Src kinases, with inhibitory effects on the proliferation of a variety of cancer cell lines, leading to G0/G1-phase blockade and apoptosis induction in BCR-ABL-expressing cells.

HG-7-85-01

😃Good

Purity: 98.08%

Catalog No. T38653Cas No. 1258391-13-7

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$68	-	In Stock
2 mg	$98	-	In Stock
5 mg	$168	-	In Stock
10 mg	$268	-	In Stock
25 mg	$538	-	In Stock
50 mg	$766	-	In Stock
100 mg	$987	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:98.08%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	HG-7-85-01 is a novel ATP-competitive and type II tyrosine kinase inhibitor targeting both wild-type and watchman mutant BCR-ABL, PDGFRα, Kit, and Src kinases, with inhibitory effects on the proliferation of a variety of cancer cell lines, leading to G0/G1-phase blockade and apoptosis induction in BCR-ABL-expressing cells.
Targets&IC50	KDR:20 nM, JAK1:120 nM, PDGFRα:440 nM, RET:30 nM, BCR-ABL (T315I):3 nM, MK5:560 nM
In vitro	HG-7-85-01 (0-1 μM; 24 hours; BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells) treatment leads to G0G1 arrest of BCR-ABL-expressing cells [1] . HG-7-85-01 (0-1 μM; 72 hours; BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells) treatment also leads to induction of apoptosis of BCR-ABL-expressing cells [1] . HG-7-85-01 treatment potently and selectively inhibits the proliferation of 32D- and Ba/F3 cells expressing nonmutant BCR-ABL and the BCR-ABL-T315I gatekeeper mutant. HG-7-85-01 shows higher potency against nonmutant BCR-ABL and BCR-ABL-T315I (IC 50 = 0.06-0.14 μM) [1] . HG-7-85-01 inhibits BCR-ABL kinase activity in a concentration-dependent manner, suggesting selective targeting of the BCR-ABL kinase as the mechanism of action of HG-7-85-01 [1] . HG-7-85-01 potently inhibits the proliferation of Ba/F3 cells expressing the Kit-T670I gatekeeper mutation (Ba/F3- Kit-T670I) and Ba/F3 cells expressing TEL/PDGFRβ and no effect on parental Ba/F3 cells. HG-7-85-01 inhibits Kit, PDGFR phosphorylation in a concentration-dependent manner [1] . The PDGFRα-T674M and PDGFRα-T674I gatekeeper mutant variants are highly responsive to HG-7-85-01 and significant IL-3 rescue [1] . HG-7-85-01 inhibits the proliferation of Ba/F3 cells transformed with human c-Src (EC 50 = 190 nM), T338I Src (EC 50 = 290 nM), and T338M Src (EC 50 = 150 nM; chicken c-Src numbering). And potently inhibits the proliferation of exon 11 Kit mutant-expressing cells, exon 9 kit mutant-expressing cells are significantly less responsive [1] . Cell Cycle Analysis [1] Cell Line: BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells Concentration: 0 μM, 0.01 μM, 0.1 μM and 1 μM Incubation Time: 24 hours Result: Led to G0G1 arrest of BCR-ABL-expressing cells. Apoptosis Analysis [1] Cell Line: BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells Concentration: 0 μM, 0.01 μM, 0.1 μM and 1 μM Incubation Time: 72 hours Result: Led to induction of apoptosis of BCR-ABL-expressing cells.
In vivo	HG-7-85-01 has limited oral bioavailability (BAV % F mouse = 5 %, rat = 19 %), a moderate half life (T 1/2 mouse =1.1 h rat = 5.8 hours), a relative low maximal serum concentration (C max mouse = 106 ng/mL at 10 mg/kg , rat = 292 ng/mL and 2 mg/kg ) and a relatively high clearance (Cl mouse = 23 ml/min/kg, rat = 13 ml/min/kg) [1] .

Chemical Properties

Molecular Weight	608.68
Formula	C₃₁H₃₁F₃N₆O₂S
Cas No.	1258391-13-7
Smiles	O=C(NC1=CC=C(C(=C1)C(F)(F)F)CN2CCN(CC)CC2)C3=CC=CC(=C3)C4=NC=5SC(=NC5C=C4)NC(=O)C6CC6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (164.29 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6429 mL	8.2145 mL	16.4290 mL	82.1450 mL
5 mM	0.3286 mL	1.6429 mL	3.2858 mL	16.4290 mL
10 mM	0.1643 mL	0.8214 mL	1.6429 mL	8.2145 mL
20 mM	0.0821 mL	0.4107 mL	0.8214 mL	4.1072 mL
50 mM	0.0329 mL	0.1643 mL	0.3286 mL	1.6429 mL
100 mM	0.0164 mL	0.0821 mL	0.1643 mL	0.8214 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc