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Size | Price | Stock |
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250mg | $1060 | Check With Us |
500mg | $1650 | Check With Us |
1g | $2475 | Check With Us |
Cat #: V0580 CAS #: 670220-88-9 Purity ≥ 98%
Description: Crenolanib (formerly also known as CP868596; RO-002; ARO-002), a benzimidazole compound, is an orally bioavailable and selective small molecule inhibitor of platelet-derived growth factor receptor (PDGFRα/β) with potential anticancer activity.
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Molecular Weight (MW) | 443.54 |
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Molecular Formula | C26H29N5O2 |
CAS No. | 670220-88-9 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 89 mg/mL (200.6 mM)r |
Water:<1 mg/mLr | |
Ethanol: 7 mg/mL (15.8 mM) | |
Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL |
SMILES Code | NC1CCN(C2=C3N=C(N4C=NC5=CC(OCC6(C)COC6)=CC=C45)C=CC3=CC=C2)CC1 |
Synonyms | RO 002; ARO 002, CP-868596; ARO-002; CP 868596; CP868596; ARO002; RO-002; RO002 |
Protocol | In Vitro | Crenolanib has 25-fold more affinity for PDGFRA/B compared with KIT, and is approximately 135-fold more potent than STI571 for inhibiting the PDGFRA D842V mutation. The IC50 for crenolanib for a KIT exon 11 deletion mutant kinase is greater than 1,000 versus 8 nM for STI571. Crenolanib has low nanomolar potency against the V561D + D842V-mutant kinase that is similar to its potency against the isolated D842V mutation. Both STI571 and crenolanib potently inhibit the kinase activity of the fusion oncogene with IC50 values of 1 and 21 nM, respectively, and inhibits PDGFRA activation in this cell line with IC50 values of 93 and 26 nM, respectively. |
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In Vivo | Crenolanib (10 mg/kg and 20 mg/kg) suppresses non-small-cell lung cancer tumor growth in vivo and induces tumor cell apoptosis, and the dosage of crenolanib applied is well tolerated by recipient mice. |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.2546 mL | 11.2729 mL | 22.5459 mL | 45.0918 mL |
5mM | 0.4509 mL | 2.2546 mL | 4.5092 mL | 9.0184 mL |
10mM | 0.2255 mL | 1.1273 mL | 2.2546 mL | 4.5092 mL |
20mM | 0.1127 mL | 0.5636 mL | 1.1273 mL | 2.2546 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.