1. Protein Tyrosine Kinase/RTK
    Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Apoptosis
  2. Bcr-Abl
    PDGFR
    c-Kit
    Src
    JAK
    Apoptosis
  3. HG-7-85-01

HG-7-85-01 

Cat. No.: HY-15814
Handling Instructions

HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.

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HG-7-85-01 Chemical Structure

HG-7-85-01 Chemical Structure

CAS No. : 1258391-13-7

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Description

HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression[1].

IC50 & Target[1]

Bcr-AblT315I

3 nM (IC50)

PDGFRα

440 nM (IC50)

KDR

20 nM (IC50)

RET

30 nM (IC50)

JAK1

120 nM (IC50)

MK5

560 nM (IC50)

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 (IC50 = 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 (EC50 = 190 nM), T338I Src (EC50 = 290 nM), and T338M Src (EC50 = 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 (T1/2 mouse =1.1 h rat = 5.8 hours), a relative low maximal serum concentration (Cmax 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].

Molecular Weight

608.68

Formula

C₃₁H₃₁F₃N₆O₂S

CAS No.

1258391-13-7

SMILES

O=C(NC1=CC=C(CN2CCN(CC)CC2)C(C(F)(F)F)=C1)C3=CC=CC(C4=CC=C5C(SC(NC(C6CC6)=O)=N5)=N4)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

HG-7-85-01Bcr-AblPDGFRc-KitSrcJAKApoptosisPlatelet-derived growth factor receptorSCFRCD117Janus kinaseATPBCR-ABLPDGFRαKDRRETDDR1tyrosinekinasescell-cycleInhibitorinhibitorinhibit

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