2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling PI3K/Akt/mTOR TGF-beta/Smad
  3. JAK Anaplastic lymphoma kinase (ALK) FLT3 STAT PI3K Akt mTOR TGF-beta/Smad TGF-β Receptor
  4. Itacnosertib hydrochloride

Itacnosertib hydrochloride  (Synonyms: TP-0184 hydrochloride)

Cat. No.: HY-109179A Purity: 99.43%
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Itacnosertib hydrochloride (TP-0184 hydrochloride) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib hydrochloride exhibits anti-leukemic activity.

For research use only. We do not sell to patients.

Itacnosertib hydrochloride Chemical Structure

Itacnosertib hydrochloride Chemical Structure

CAS No. : 2409543-84-4

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Based on 1 publication(s) in Google Scholar

Other Forms of Itacnosertib hydrochloride:

Itacnosertib hydrochloride Related Antibodies

Top Publications Citing Use of Products

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JAK1 JAK2 JAK3 Tyk2 JAK

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STAT3 STAT5 STAT6 STAT1

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • Biological Activity

  • Purity & Documentation

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Description

Itacnosertib hydrochloride (TP-0184 hydrochloride) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib hydrochloride exhibits anti-leukemic activity[1][2].

IC50 & Target[2]

ACVR1

8 nM (IC50)

JAK2

8540 nM (IC50)

In Vitro

Itacnosertib hydrochloride (0-200 nM, 24-48 h) arrests the cell cycle of MOLM-13, MOLM-14 and MV4-11 at G1/G0 phase, inhibits the proliferation of acute myeloid leukemia (AML) cells, IC50s for MOLM-13, MOLM-14 and MV4-11 (FLT3-mutated AML cells) are 6.4, 1.2 and 1.3 nM, respectively. Itacnosertib hydrochloride inhibits the AML FLT3-wildtype cell with IC50 > 100 nM[2].
Itacnosertib hydrochloride inhibits the activation of FLT3 and ACVR1 downstream signaling pathways, inhibits serine biosynthesis and amino acid transport pathways[2].

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

Itacnosertib hydrochloride Related Antibodies

Western Blot Analysis[2]

Cell Line: MOLM-13, MOLM-14 and MV4-11
Concentration: 0-1000 nM
Incubation Time: 24-48 h
Result: Inhibited the phosphorylation of STAT5, MKK3, ERK, PI3K, AKT, mTOR, p-4E-BP1, p-S6K and SMAD1/5.

Cell Cycle Analysis[2]

Cell Line: MOLM-13, MOLM-14 and MV4-11
Concentration: 0-200 nM
Incubation Time: 24-48 h
Result: Arrested the cell cycle at subG1 phase.
In Vivo

Itacnosertib hydrochloride (50-200 mg/kg, po, once weekly for 5-6 weeks) exhibits antitumor activity against MOLM-13 in mouse models[2].

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

Animal Model: Mouse MOLM-13 xenograft models[2]
Dosage: 50-200 mg/kg
Administration: po, once weekly for 5-6 weeks
Result: Inhibited the leukemia growth, prolonged the mice survival.
Molecular Weight

505.01

Formula

C26H29ClN8O
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

CN1CCN(C2=CC=C(NC3=NC=CC(NC4=CC=CN=C4C5=NC=CC=C5)=N3)C=C2OC)CC1.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 5.56 mg/mL (11.01 mM; ultrasonic and warming and heat to 60°C; 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 1.9802 mL 9.9008 mL 19.8016 mL
5 mM 0.3960 mL 1.9802 mL 3.9603 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 (sealed storage, away from moisture). 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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 (sealed storage, away from moisture). 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 1.9802 mL 9.9008 mL 19.8016 mL 49.5040 mL
5 mM 0.3960 mL 1.9802 mL 3.9603 mL 9.9008 mL
10 mM 0.1980 mL 0.9901 mL 1.9802 mL 4.9504 mL
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Itacnosertib hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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:

Itacnosertib2409543-84-4TP-0184TP0184TP 0184JAKAnaplastic lymphoma kinase (ALK)FLT3STATPI3KAktmTORTGF-beta/SmadTGF-β ReceptorJanus kinaseAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Phosphoinositide 3-kinasePKBProtein kinase BMammalian target of RapamycinTransforming growth factor betaTransforming growth factor beta receptorsJAK2/ACVR1 (ALK2)/ALK5 inhibitorCancerInhibitorinhibitorinhibit

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