CAL-130PI3K inhibitor CAS# 1431697-74-3 |
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Quality Control & MSDS
3D structure
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| Cas No. | 1431697-74-3 | SDF | Download SDF |
| PubChem ID | 71576676 | Appearance | Powder |
| Formula | C23H22N8O | M.Wt | 426.47 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO | ||
| Chemical Name | 2-[(1S)-1-[(2-amino-7H-purin-6-yl)amino]ethyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one | ||
| SMILES | CC1=C2C(=CC=C1)N=C(N(C2=O)C3=CC=CC=C3C)C(C)NC4=NC(=NC5=C4NC=N5)N | ||
| Standard InChIKey | PUYVJBBSBPUKBT-AWEZNQCLSA-N | ||
| Standard InChI | InChI=1S/C23H22N8O/c1-12-7-4-5-10-16(12)31-21(28-15-9-6-8-13(2)17(15)22(31)32)14(3)27-20-18-19(26-11-25-18)29-23(24)30-20/h4-11,14H,1-3H3,(H4,24,25,26,27,29,30)/t14-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.In Vitro:CAL-130 preferentially inhibits the function of both p110γ and p110δ catalytic domains. IC50 values of CAL-130 are 1.3 and 6.1 nM for p110δ and p110γ, respectively, as compared to 115 and 56 nM for p110α and p110β. CAL-130 does not inhibit additional intracellular signaling pathways (i.e., p38 MAPK or insulin receptor tyrosine kinase) that are critical for general cell function and survival[1].In Vivo:The clinical significance of interfering with the combined activities of PI3Kγ and PI3Kδ is determined by administering CAL-130 to Lck/Ptenfl/fl mice with established T cell acute lymphoblastic leukemia (T-ALL). Candidate animals for survival studies are ill appearing, have a white blood cell (WBC) count above 45,000 μL-1, evidence of blasts on peripheral smear, and a majority of circulation cells (>75%) staining double positive for Thy1.2 and Ki-67. Mice receive an oral dose (10 mg/kg) of CAL-130 every 8 hr for a period of 7 days and are then followed until moribund. Despite the limited duration of therapy, CAL-130 is highly effective in extending the median survival for treated animals to 45 days as compared 7.5 days for the control group[1]. References: | |||||
CAL-130 Dilution Calculator
CAL-130 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3448 mL | 11.7242 mL | 23.4483 mL | 46.8966 mL | 58.6208 mL |
| 5 mM | 0.469 mL | 2.3448 mL | 4.6897 mL | 9.3793 mL | 11.7242 mL |
| 10 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 4.6897 mL | 5.8621 mL |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.469 mL | 0.9379 mL | 1.1724 mL |
| 100 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.469 mL | 0.5862 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Class I phosphoinositide 3-kinase (PI3K) activate fundamental pathways controlling cell survival, metabolism, proliferation and and therefore play crucial role in cancer development. It is reported that p110γ is mainly expressed in leukocytes, whose role in cancer development is recently starting to be studied. CAL-130 is a specific dual inhibitor of p110γ and p110δ.
In vitro: To demonstrate that CAL-130 can block the activities of both PI3Kγ and PI3Kδ in thymocytes, previous autors evaluated its ability of preventing phosphorylation of Akt (Ser473) and calcium flux in response to T cell receptor (TCR). Consistently, CAL-130 treated thymocytes from 6-week-old WT animals prevented TCR-induced Akt phosphorylation and attenuated calcium flux to levels observed for their Pik3cγ-/-; Pik3cδ-/- counterparts [1].
In vivo: To assess the in vivo efficacy, previous study determined its effects on 6-week-old WT mice thymi. Mice orally received 10 mg/kg of the inhibitor, which was sufficient to maintain plasma concentrations of 0.33 μM at the end of 8 hrs. Moreover, such dose did not affect either plasma glucose or insulin levels. In contrast, CAL-130 treatment (10 mg/kg every 8 hrs) for a period of 7 days greatly affected the size, cellularity, and overall architecture of the thymus. Notely there was a 18-fold reduction in total thymocyte number when comparred to controls, which was mainly due to the DP population loss [1].
Clinical trial: CAL-130 is currently in the preclinical developlent stage and no clinical data are available.
Reference:
[1] Subramaniam PS, Whye DW, Efimenko E, Chen J, Tosello V, De Keersmaecker K, Kashishian A, Thompson MA, Castillo M, Cordon-Cardo C, Davé UP, Ferrando A, Lannutti BJ, Diacovo TG. Targeting nonclassical oncogenes for therapy in T-ALL. Cancer Cell. 2012;21(4):459-72.
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Targeting nonclassical oncogenes for therapy in T-ALL.[Pubmed:22516257]
Cancer Cell. 2012 Apr 17;21(4):459-72.
Constitutive phosphoinositide 3-kinase (PI3K)/Akt activation is common in T cell acute lymphoblastic leukemia (T-ALL). Although four distinct class I PI3K isoforms (alpha, beta, gamma, delta) could participate in T-ALL pathogenesis, none has been implicated in this process. We report that in the absence of PTEN phosphatase tumor suppressor function, PI3Kgamma or PI3Kdelta alone can support leukemogenesis, whereas inactivation of both isoforms suppressed tumor formation. The reliance of PTEN null T-ALL on the combined activities of PI3Kgamma/delta was further demonstrated by the ability of a dual inhibitor to reduce disease burden and prolong survival in mice as well as prevent proliferation and promote activation of proapoptotic pathways in human tumors. These results support combined inhibition of PI3Kgamma/delta as therapy for T-ALL.
