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

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

HG-7-85-01 構造式

CAS 番号 : 1258391-13-7

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5 mg $205 在庫あり
10 mg $325 在庫あり
25 mg $650 在庫あり
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HG-7-85-01 関連抗体

Top Publications Citing Use of Products

Bcr-Abl アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Abl Bcr-Abl

PDGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PDGFR PDGFRβ PDGFRα

Src アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

JAK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
JAK1 JAK2 JAK3 Tyk2 JAK

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製品説明

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

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)

Cellular Effect
Cell Line Type Value Description References
BaF3 EC50
0.156 μM
Compound: 22, HG-7-85-01
Cytotoxicity against mouse BA/F3 cells expressing imatinib resistant Bcr-Abl T3151 mutant
Cytotoxicity against mouse BA/F3 cells expressing imatinib resistant Bcr-Abl T3151 mutant
[PMID: 22819762]
BaF3 EC50
3.085 μM
Compound: 22, HG-7-85-01
Cytotoxicity against mouse BA/F3 cells expressing wild type Bcr-Abl
Cytotoxicity against mouse BA/F3 cells expressing wild type Bcr-Abl
[PMID: 22819762]
BaF3 EC50
3.085 μM
Compound: 22, HG-7-85-01
Cytotoxicity against wild type mouse BA/F3 cells
Cytotoxicity against wild type mouse BA/F3 cells
[PMID: 22819762]
体外実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HG-7-85-01 関連抗体

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.
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

608.68

分子式

C31H31F3N6O2S
CAS 番号
Appearance

Solid

Color

White to off-white

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 125 mg/mL (205.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6429 mL 8.2145 mL 16.4290 mL
5 mM 0.3286 mL 1.6429 mL 3.2858 mL
10 mM 0.1643 mL 0.8214 mL 1.6429 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6429 mL 8.2145 mL 16.4290 mL 41.0725 mL
5 mM 0.3286 mL 1.6429 mL 3.2858 mL 8.2145 mL
10 mM 0.1643 mL 0.8214 mL 1.6429 mL 4.1072 mL
15 mM 0.1095 mL 0.5476 mL 1.0953 mL 2.7382 mL
20 mM 0.0821 mL 0.4107 mL 0.8214 mL 2.0536 mL
25 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6429 mL
30 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3691 mL
40 mM 0.0411 mL 0.2054 mL 0.4107 mL 1.0268 mL
50 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8214 mL
60 mM 0.0274 mL 0.1369 mL 0.2738 mL 0.6845 mL
80 mM 0.0205 mL 0.1027 mL 0.2054 mL 0.5134 mL
100 mM 0.0164 mL 0.0821 mL 0.1643 mL 0.4107 mL
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HG-7-85-01 Related Classifications

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HG-7-85-011258391-13-7Bcr-AblPDGFRc-KitSrcJAKApoptosisPlatelet-derived growth factor receptorSCFRCD117Janus kinaseATPBCR-ABLPDGFRαKDRRETDDR1tyrosinekinasescell-cycleInhibitorinhibitorinhibit

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