Size | Price | |
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10mg | ||
25mg | ||
50mg | ||
100mg | ||
250mg |
Purity: ≥98%
CAL-130 is a novel, potent and selective PI3Kδ and PI3Kγ inhibitor with potential anticancer activity and with IC50s of 1.3 and 6.1 nM, respectively. Constitutive phosphoinositide 3-kinase (PI3K)/Akt activation is common in T cell acute lymphoblastic leukemia (T-ALL). Although four distinct class I PI3K isoforms (α, β, γ, δ) could participate in T-ALL pathogenesis, none has been implicated in this process. In the absence of PTEN phosphatase tumor suppressor function, PI3Kγ or PI3Kδ alone can support leukemogenesis, whereas inactivation of both isoforms suppressed tumor formation.
ln Vitro |
The catalytic domains of p110γ and p110δ are preferentially inhibited by CAL-130; the IC50 values of CAL-130 for p110δ and p110η were 1.3 and 6.1 nM, respectively, while the IC50 values for p110α and p110β were 115 and 56 nM, respectively. Other intracellular signaling pathways, such as p38 MAPK or insulin receptor tyrosine kinase, that are essential for general cellular function and survival, are not inhibited by CAL-130 [1].
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ln Vivo |
Interfering with the combined activities of PI3Kγ and PI3Kδ was found to have clinical significance when given to Lck/Ptenfl/fl mice that had T-cell acute lymphoblastic leukemia (T-ALL). The animals considered for survival studies are not well-groomed, their white blood cell (WBC) counts are higher than 45,000 μL-1, peripheral smears show blast activity, and most circulating cells (>75%) are Thy1.2 and Thy1-sensitive. 2 Positive staining twice. Base-67. Oral CAL-130 (10 mg/kg) was given to mice every 8 hours for 7 days, after which they were monitored until they became moribund. The median survival of treated animals was extended to 45 days by CAL-130, despite the short treatment duration, as opposed to 7.5 days for the control group [1].
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References |
[1]. Subramaniam Prem S, et al. Targeting nonclassical oncogenes for therapy in T-ALL. Cancer cell (2012), 21(4), 459-72
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Molecular Formula |
C23H22N8O
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Molecular Weight |
426.474
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CAS # |
1431697-74-3
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Related CAS # |
CAL-130 Hydrochloride;1431697-78-7;CAL-130 Racemate;474012-90-3
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SMILES |
O=C1N(C2=CC=CC=C2C)C([C@H](C)NC3=C4N=CNC4=NC(N)=N3)=NC5=C1C(C)=CC=C5
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Synonyms |
CAL130; CAL 130; CAL-130
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3448 mL | 11.7242 mL | 23.4483 mL | |
5 mM | 0.4690 mL | 2.3448 mL | 4.6897 mL | |
10 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(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.