Name: ABL001 (Asciminib)
Brand: Selleck Chemicals
SKU: S8555
Availability: InStock
Rating: 5 (16 reviews)

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Quality Control

Batch: Purity: 99.88%

99.88

Related Targets	EGFR VEGFR JAK FGFR PDGFR Src HIF FLT3 HER2 FLT
Other Bcr-Abl Inhibitors	Degrasyn (WP1130) Bafetinib (INNO-406) Rebastinib (DCC-2036) GNF-5 Berbamine GNF-2 Olverembatinib dimesylate (GZD824) PD173955 GNF-7 Berbamine dihydrochloride

Solubility

In vitro
Batch:

DMSO : 89 mg/mL (197.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 89 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.500mg/ml (10.00mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.550mg/ml (1.22mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	449.84	Formula	C₂₀H₁₈ClF₂N₅O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1492952-76-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			SMILES	C1CN(CC1O)C2=C(C=C(C=N2)C(=O)NC3=CC=C(C=C3)OC(F)(F)Cl)C4=CC=NN4

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	Abl1 (Cell-free assay) 0.45 nM
In vitro	Asciminib (ABL001) is a potent, selective BCR-ABL inhibitor that maintains activity across most mutations, including T315I, with a distinct, allosteric mechanism of action. It binds at a regulatory site typically occupied by a myristoyl group in wild-type ABL and inhibits ABL kinase activity through a mechanism distinct from catalytic site inhibitors. This compound binds to a pocket on the BCR-ABL kinase domain that is normally occupied by the myristoylated N-terminus of ABL1. Upon fusion with BCR, this myristoylated N-terminus that serves to autoregulate ABL1 activity is lost. ABL001 functionally mimics the role of the myristoylated N-terminus by occupying its vacant binding site and restores the negative regulation of the kinase activity. It selectively inhibits the growth of chronic myelogenous leukemia (CML) and Ph+ ALL cells with potencies ranging from 1-10 nM range while BCR-ABL-negative cell lines remained unaffected at concentrations 1000-fold higher. NMR and biophysical studies confirm that it binds potently (dissociation constant (Kd) = 0.5-0.8 nM) and selectively to the myristoyl pocket of ABL1 and induces the inactive C-terminal helix conformation. This compound lacks activity against more than 60 kinases, including SRC and is similarly inactive against G-protein-coupled receptors, ion channels, nuclear receptors and transporters. Thus, it has high selectivity.
In vivo	In the KCL-22 mouse xenograft model, Asciminib (ABL001) displays potent anti-tumor activity with complete tumor regression observed and a clear dose-dependent correlation with pSTAT5 inhibition. It has moderate oral absorption, volume of distribution and half-life across all species. This compound as a single agent induces clinical anti-tumour activity and is well tolerated to date in a heavily pre-treated subgroup of patients with chronic myelogenous leukemia. As for the pharmacokinetics, pharmacodynamics and efficacy, the CL (clearance) are 12, 16 and 6 mL/min/kg in mice, rats and dogs after a single iv dose of 1mg/kg, 2mg/kg and 1mg/kg, respectively. In mouse and dog, the T_1/2term are 1.1 and 3.7 h after a single i.v. dose at 1 mg/kg. In Rat, the T_1/2term is 2.7 h after a single i.v. dose at 2 mg/kg. The oral bioavailability in mouse and rat are 35% and 27% respectively when dosed at 30 mg/kg p.o. While in dogs the oral BA is 111% (15 mg/kg, p.o).
References	[1] http://www.bloodjournal.org/content/124/21/398?sso-checked=true [2] http://clincancerres.aacrjournals.org/content/23/1_Supplement/IA01 [3] https://www.nature.com/articles/nature21702

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-03-25)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07493408	NOT_YET_RECRUITING	Ph+ Acute Lymphoblastic Leukemia (Ph+ALL); Blastic Transformation of Chronic Myeloid Leukemia; Philadelphia Chromosome-positive B-cell Acute Lymphoblastic Leukemia (Ph+ B-ALL); Haematopoietic Stem Cell Transplant, Allogeneic	The University of Hong Kong	2026-03-30	PHASE2
NCT07387926	RECRUITING	Acute Lymphoblastic Leukemia; Leukemia, Lymphoblastic, Acute, Philadelphia-Positive; Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia	Novartis Pharmaceuticals	2026-07-05	PHASE1; PHASE2
NCT06236724	RECRUITING	Chronic Myeloid Leukemia	M.D. Anderson Cancer Center	2024-01-31	PHASE2
NCT07354074	RECRUITING	Chronic Myelogenous Leukemia; Leukemia, Myelogenous, Chronic, Philadelphia Chromosome Positive	Novartis Pharmaceuticals	2026-04-28	PHASE2
NCT05143840	ACTIVE_NOT_RECRUITING	Chronic Myeloid Leukemia, Chronic Phase; Adult CML; Leukemia, Myeloid; Leukemia,Myeloid, Chronic	University of Alabama at Birmingham	2022-04-22	PHASE2
NCT07604233	NOT_YET_RECRUITING	Myeloid Leukemia	M.D. Anderson Cancer Center	2026-11-30	PHASE1; PHASE2

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ABL001 (Asciminib) STAMP Inhibitor

Chemical Structure

Molecular Weight: 449.84