Asciminib HCl
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $950 | Check With Us |
| 500mg | $1500 | Check With Us |
| 1g | $2250 | Check With Us |
: Cat #: V6496 CAS #: 2119669-71-3 Purity ≥ 99%
Description: Asciminib HCl (ABL001; ABL-001; Scemblix), the hydrochloride salt of Asciminib, is an allosteric inhibitor of BCR-ABL1 that has been approved FDA on Oct 29th 2021 for treating Philadelphia chromosome-positive CML (chronic myeloid leukemia).
Top Publications Citing Invivochem Products
Publications Citing InvivoChem Products
Product Promise
- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 486.30 |
|---|---|
| Molecular Formula | C20H19Cl2F2N5O3 |
| CAS No. | 2119669-71-3 |
| SMILES Code | O=C(C1=CC(C2=NNC=C2)=C(N3C[C@H](O)CC3)N=C1)NC4=CC=C(OC(F)(Cl)F)C=C4.[H]Cl |
| Synonyms | ABL-001; AB -001; ABL001; asciminib Asciminib hydrochloride; ABL001-AAA; |
| Protocol | In Vitro | Asciminib hydrochloride is selectively active against all BCR–ABL1 lines (IC50 value of 1–20 nM), irrespective of the presence of either the p210 or the p190 BCR–ABL1 isoform. In BCR–ABL1-transformed Ba/F3 cells grown without IL-3, Asciminib hydrochloride has an anti-proliferative with IC50 value of 0.25 nM. In the CML blast-phase cell line KCL-22, Asciminib hydrochloride inhibits phosphorylation of both STAT5 (Tyr694; pSTAT5) and BCR–ABL1 (Tyr245; pBCR–ABL1) after 1 h using concentrations that correlate with those required for inhibition of cell proliferation. Asciminib hydrochloride lacks activity against more than 60 kinases, including SRC, and is similarly inactive against G-protein-coupled receptors, ion channels, nuclear receptors and transporters. Asciminib hydrochloride binds potently (dissociation constant=0.5-0.8 nM) and selectively to the myristoyl pocket of ABL1 and induces the inactive C-terminal helix conformation. Asciminib hydrochloride exhibits the same non-ATP-competitive biochemical kinetics as the BCR–ABL inhibitor GNF-2 but with approximately 100-fold greater potency. Asciminib (ABL001) hydrochloride binds to the myristoyl pocket of ABL1 and induces the formation of an inactive kinase conformation. |
|---|---|---|
| In Vivo | Single doses of 7.5, 15 and 30 mg/kg Asciminib, administered to mice bearing KCL- 22 xenografts, inhibits pSTAT5 (Tyr694), which return to baseline at 10, 12 and 16-20 h 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.0563 mL | 10.2817 mL | 20.5634 mL | 41.1269 mL |
| 5mM | 0.4113 mL | 2.0563 mL | 4.1127 mL | 8.2254 mL |
| 10mM | 0.2056 mL | 1.0282 mL | 2.0563 mL | 4.1127 mL |
| 20mM | 0.1028 mL | 0.5141 mL | 1.0282 mL | 2.0563 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
Concentration(final)
×
Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
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 add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.