Cat. No.: HY-104010

Asciminib

(Synonyms: ABL001)

16 Cited Publications

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Based on 16 publication(s) in Google Scholar

Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC₅₀ of 0.25 nM.

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Pureté: 99.61%
CAS No.: 1492952-76-7
Formule: C₂₀H₁₈ClF₂N₅O₃
Masse moléculaire:449.84

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Asciminib Chemical Structure

CAS No.: 1492952-76-7

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (16)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC₅₀ of 0.25 nM^[1].

Voir tous les produits spécifiques à Isoform Bcr-Abl :

Abl
Bcr-Abl

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	>10000 nM Compound: 1; ABL001	Cytotoxicity against mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by BriteLight luciferase assay Cytotoxicity against mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by BriteLight luciferase assay	[PMID: 30137981]
BaF3	EC₅₀	>10 μM Compound: Asciminib; ABL001	Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay	[PMID: 32657579]
BaF3	EC₅₀	5.8 nM Compound: Asciminib; ABL001	Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay	[PMID: 32657579]
BaF3	IC₅₀	0.012 μM Compound: ABL001	Antiproliferative activity against mouse BaF3 cells expressing Bcr-Abl T315I mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells expressing Bcr-Abl T315I mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 35561654]
HEK293	IC₅₀	>10 μM Compound: Asciminib	Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by alamar blue assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by alamar blue assay	[PMID: 35944901]
K562	IC₅₀	0.61 nM Compound: Asciminib; ABL001	Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay	[PMID: 32657579]
K562	IC₅₀	3.9 nM Compound: ABL001	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 2 days by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 2 days by CCK8 assay	[PMID: 36306539]
K562	EC₅₀	0.26 nM Compound: Asciminib	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 3 days in the presence of dasatinib by celltiter-glo 2.0 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 3 days in the presence of dasatinib by celltiter-glo 2.0 assay	[PMID: 37849551]
K562	EC₅₀	0.39 nM Compound: Asciminib	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 3 days in the presence of ponatinib by celltiter-glo 2.0 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 3 days in the presence of ponatinib by celltiter-glo 2.0 assay	[PMID: 37849551]
K562	EC₅₀	1.49 nM Compound: Asciminib	Antiproliferative activity against human K562 cells expressing ABL T315I mutant assessed as inhibition of cell growth incubated for 3 days in the presence of ponatinib by celltiter-glo 2.0 assay Antiproliferative activity against human K562 cells expressing ABL T315I mutant assessed as inhibition of cell growth incubated for 3 days in the presence of ponatinib by celltiter-glo 2.0 assay	[PMID: 37849551]
K562	EC₅₀	11.99 nM Compound: Asciminib	Antiproliferative activity against human K562 cells expressing ABL T315I mutant assessed as inhibition of cell growth incubated for 3 days in the presence of dasatinib by celltiter-glo 2.0 assay Antiproliferative activity against human K562 cells expressing ABL T315I mutant assessed as inhibition of cell growth incubated for 3 days in the presence of dasatinib by celltiter-glo 2.0 assay	[PMID: 37849551]
K562	EC₅₀	7.59 nM Compound: Asciminib	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo 2.0 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo 2.0 assay	[PMID: 37849551]
K562	EC₅₀	88.07 nM Compound: Asciminib	Antiproliferative activity against human K562 cells expressing ABL T315I mutant assessed as inhibition of cell growth incubated for 3 days by celltiter-glo 2.0 assay Antiproliferative activity against human K562 cells expressing ABL T315I mutant assessed as inhibition of cell growth incubated for 3 days by celltiter-glo 2.0 assay	[PMID: 37849551]

In Vitro

Asciminib binds to the myristoyl pocket of ABL1 and induces the formation of an inactive kinase conformation. NMR and biophysical studies confirm that asciminib binds potently (dissociation constant=0.5-0.8nM) and selectively to the myristoyl pocket of ABL1 and induces the inactive C-terminal helix conformation. Asciminib binding mimics the structural consequences of myristate binding to the N terminus of ABL1. Consistent with this binding site, asciminib exhibits the same non-ATP-competitive biochemical kinetics as the BCR–ABL inhibitor GNF-2 but with approximately 100-fold greater potency. Asciminib lacks activity against more than 60 kinases, including SRC, and is similarly inactive against G-protein-coupled receptors, ion channels, nuclear receptors and transporters. In BCR–ABL1-transformed Ba/F3 cells grown without IL-3, asciminib has an anti-proliferative with IC₅₀ value of 0.25nM. In the CML blast-phase cell line KCL-22, asciminib inhibits phosphorylation of both STAT5 (Tyr694; pSTAT5) and BCR–ABL1 (Tyr245; pBCR–ABL1) after 1h using concentrations that correlate with those required for inhibition of cell proliferation. Asciminib is selectively active against all BCR–ABL1 lines (IC₅₀ value of 1–20nM), irrespective of the presence of either the p210 or the p190 BCR–ABL1 isoform.^[1].

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

In Vivo

Asciminib is undergoing clinical development testing in patients with CML and Philadelphia chromosome-positive acute lymphoblastic leukaemia. Single doses of 7.5, 15 and 30 mg/kg ABL001, administered to mice bearing KCL- 22 xenografts, inhibits pSTAT5 (Tyr694), which return to baseline at 10, 12 and 16-20h after administration of the dose, respectively. In mice implanted with KCL-22 tumors, the minimum dose of asciminib required for complete regression is 7.5 mg/kg twice a day (BID) or 30 mg/kg once a day (QD), and is tolerated at doses up to 250 mg/kg BID. Similarly, in xenografts derived from patients, treatment with 7.5 and 30 mg/kg asciminib leads to regressions that are maintained during dosing^[1].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1492952-76-7
Appearance Solid
Masse moléculaire 449.84
Formule C₂₀H₁₈ClF₂N₅O₃
Color White to off-white
SMILES

O=C(C1=CC(C2=NNC=C2)=C(N3C[C@H](O)CC3)N=C1)NC4=CC=C(OC(F)(Cl)F)C=C4
Synonyms

ABL001
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (16)

All Flow CytometryCell Proliferation/Viability AssayIFIn Vivo Efficacy StudyHistological Imaging/Staining

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Journal Impact Factor

Nature

Inhibitors supercharge kinase turnover through native proteolytic circuits. [Abstract]

2026 Jan;649(8098):1032-1041. PMID: 41299171

Asciminib purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1032-1041. [Abstract]

KBM7 iCas9 stability reporter validation for dose-dependent stabilization using Asciminib (10^-10-10^-4 M) for either ABL1^WT or ABL1^C464W constructs measured by flow cytometry.
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Autophagy

Nonreceptor tyrosine kinase ABL1 regulates lysosomal acidification by phosphorylating the ATP6V1B2 subunit of the vacuolar-type H+-ATPase. [Abstract]

2025 Jun;21(6):1192-1211. PMID: 39757940

Asciminib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jun;21(6):1192-1211. [Abstract]

Asciminib (10 μM) caused significant accumulation of mitochondria in lysosomes of CCC-HEH-2 (human embryonic myocardial tissue derived) cells treated with CCCP.

Asciminib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jun;21(6):1192-1211. [Abstract]

Asciminib (30 mg/kg; i.g.; 6 weeks) resulted in significantly impaired cardiac function in C57BL/6J mice.

Asciminib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jun;21(6):1192-1211. [Abstract]

Asciminib (30 mg/kg; i.g.; 6 weeks) increased the colocalization of mitochondria with lysosomes in cardiac sections of C57BL/6J mice.

Asciminib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jun;21(6):1192-1211. [Abstract]

Asciminib (5-10 μM) caused a higher GFP:RFP ratio in the lysosomes of WT A549 cells stably transfected with a puromycin-inducible stubRFP-sensGFP-LC3 lentivirus.
Adv Sci (Weinh)

BCR::ABL1-Induced Enhancer Reprogramming Uncovers Hypersensitivity of Ph+B-ALL Cells to Enhancer-Targeting Drugs. [Abstract]

2026 Mar 1:e17231. PMID: 41764406
Leukemia

BCR::ABL1 tyrosine kinase inhibitors induce ribosome collisions to activate ZAK-dependent ribotoxic stress and apoptosis in chronic myeloid leukemia. [Abstract]

2026 May;40(5):955-969. PMID: 41912913
Cell Death Dis

Combination of tyrosine kinase inhibitors and the MCL1 inhibitor S63845 exerts synergistic antitumorigenic effects on CML cells. [Abstract]

2021 Sep 25;12(10):875. PMID: 34564697
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Cancer Immunol Immunother

Effects of the STAMP-inhibitor asciminib on T cell activation and metabolic fitness compared to tyrosine kinase inhibition by imatinib, dasatinib, and nilotinib. [Abstract]

2023 Jun;72(6):1661-1672. PMID: 36602564

Asciminib purchased from MedChemExpress. Usage Cited in: Cancer Immunol Immunother. 2023 Jun;72(6):1661-1672. [Abstract]

Asciminib (1.25, 5, 10 µM) inhibits proliferation of T cells.
Cancer Sci

CML With Mutant ASXL1 Showed Decreased Sensitivity to TKI Treatment via Upregulation of the ALOX5-BLTR Signaling Pathway. [Abstract]

2025 Apr;116(4):1115-1125. PMID: 39905783
Sci Rep

Neddylation status determines the therapeutic sensitivity of tyrosine kinase inhibitors in chronic myeloid leukemia. [Abstract]

2025 May 30;15(1):18978. PMID: 40447744
J Biol Chem

Allosteric enhancement of the BCR-Abl1 kinase inhibition activity of nilotinib by cobinding of asciminib. [Abstract]

2022 Aug;298(8):102238. PMID: 35809644
BMC Cancer

The effects of combination treatments on drug resistance in chronic myeloid leukaemia: an evaluation of the tyrosine kinase inhibitors axitinib and asciminib. [Abstract]

2020 May 7;20(1):397. PMID: 32380976
Blood Vessel Thromb Hemost

2025 Nov 17.
bioRxiv

Phosphorylation-inducing chimera rewires oncogenic kinase to trigger apoptosis. [Abstract]

2025 Jun 13:2025.06.13.659082. PMID: 40661463
bioRxiv

A Hotspot Phosphorylation Site on SHP2 Drives Oncoprotein Activation and Drug Resistance. [Abstract]

2025 Jun 16:2025.06.11.659120. PMID: 40667115
bioRxiv

2025 Jan 30.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (222.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2230 mL

11.1151 mL

22.2301 mL

5 mM

0.4446 mL

2.2230 mL

4.4460 mL

10 mM

0.2223 mL

1.1115 mL

2.2230 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

Ba/F3 cells are treated with a range concentration of asciminib (0-10000 nM) for 48 h. Cell proliferation is measured using the Britelite luciferase detection assay^[1].

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

Animal Administration^[1]

Mice: Asciminib efficacy in three patient-derived ALL systemic xenograft models (ALL-7015, AL-7119 and AL-7155) is assessed by FACS monitoring of the percentage of CD45+ cells per live cell in blood samples taken at varying time points after dosing with either 7.5 mg/kg BID (group 2) or 30 mg/kg BID (group 3) asciminib for 3 weeks^[1].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Wylie AA, et al. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1. Nature. 2017 Mar 30;543(7647):733-737. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.2230 mL	11.1151 mL	22.2301 mL	55.5753 mL
	5 mM	0.4446 mL	2.2230 mL	4.4460 mL	11.1151 mL
	10 mM	0.2223 mL	1.1115 mL	2.2230 mL	5.5575 mL
	15 mM	0.1482 mL	0.7410 mL	1.4820 mL	3.7050 mL
	20 mM	0.1112 mL	0.5558 mL	1.1115 mL	2.7788 mL
	25 mM	0.0889 mL	0.4446 mL	0.8892 mL	2.2230 mL
	30 mM	0.0741 mL	0.3705 mL	0.7410 mL	1.8525 mL
	40 mM	0.0556 mL	0.2779 mL	0.5558 mL	1.3894 mL
	50 mM	0.0445 mL	0.2223 mL	0.4446 mL	1.1115 mL
	60 mM	0.0371 mL	0.1853 mL	0.3705 mL	0.9263 mL
	80 mM	0.0278 mL	0.1389 mL	0.2779 mL	0.6947 mL
	100 mM	0.0222 mL	0.1112 mL	0.2223 mL	0.5558 mL

Keywords

Asciminib

16 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Asciminib

Voir tous les produits spécifiques à Isoform Bcr-Abl

Activité biologique

Chemical Information

Publications (16)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Asciminib Related Classifications

HY-104010 Related Classifications