CAL-130 Hydrochloride

Cat. No.: HY-16122B Purity: 98.74%: FAQs
Data Sheet SDS COA Handling Instructions

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CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC₅₀s of 1.3 and 6.1 nM, respectively.

For research use only. We do not sell to patients.

CAL-130 Hydrochloride Chemical Structure

CAS No. : 1431697-78-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 290	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 290	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 264	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1195	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Other Forms of CAL-130 Hydrochloride:

CAL-130 Racemate Get quote
CAL-130 Get quote

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•Related Screening Libraries:

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View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC₅₀s of 1.3 and 6.1 nM, respectively.

IC₅₀ & Target^[1]

p110δ

1.3 nM (IC₅₀)

p110γ

6.1 nM (IC₅₀)

p110β

56 nM (IC₅₀)

p110α

115 nM (IC₅₀)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The clinical significance of interfering with the combined activities of PI3Kγ and PI3Kδ is determined by administering CAL-130 to Lck/Pten^fl/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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

462.93

Formula

C₂₃H₂₃ClN₈O

CAS No.

1431697-78-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C2=CC=CC=C2C)C([C@H](C)NC3=C4N=CNC4=NC(N)=N3)=NC5=C1C(C)=CC=C5.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (108.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1602 mL	10.8008 mL	21.6015 mL
5 mM	0.4320 mL	2.1602 mL	4.3203 mL
10 mM	0.2160 mL	1.0801 mL	2.1602 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (6.48 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (6.48 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (6.48 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.74%

Select Batch:

Data Sheet (292 KB) SDS (251 KB)

COA (254 KB) HNMR (282 KB) RP-HPLC (206 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[1]. Subramaniam Prem S, et al. Targeting nonclassical oncogenes for therapy in T-ALL. Cancer cell (2012), 21(4), 459-72. [Content Brief]

Kinase Assay ^[1]	IC₅₀ values for CAL-130 inhibition of PI3K isoforms are determined in ex vivo PI3 kinase assays using recombinant PI3K. A ten-point kinase inhibitory profile is determined with ATP at a concentration consistent with the K_M for each enzyme^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cell proliferation of CCRF-CEM cells or shRNA-transfected CCRF-CEM cells, in presence or absence of CAL-130 (1, 2.5 and 5 μM), is followed by cell counting of samples in triplicate using a hemocytometer and trypan blue. For apoptosis determinations of untransfected or shRNA-transfected CCRF-CEMs, cells are stained with APC-conjugated Annexin-V in Annexin Binding Buffer and analyzed by flow cytometry. For primary T-ALL samples, cell viability is assessed using the BD Cell Viability kit coupled with the use of fluorescentcounting beads. For this, cells are plated with MS5-DL1 stroma cells, and after 72 hr following CAL-130 treatment, cells are harvested and stained with an APC-conjugated antihuman CD45 followed by a staining with the aforementioned kit^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] For subcutaneous xenograft experiments, luminescent CCRF-CEM (CEMluc) cells are generated by lentiviral infection with FUW-luc and selection with Neomycin. Luciferase expression is verified with the Dual-Luciferase Reporter Assay kit. 2.5×10⁶ CEM-luc cells embedded in Matrigel are injected in the flank of *NOD.Cg-Prkdc^scid* Il2rg^tm1Wjl/Sz mice. After 1 week, mice are treated by oral gavage with vehicle (0.5% methyl cellulose, 0.1% Tween 80), or CAL-130 (10 mg/kg) every 8 hr daily for 4 days*, and then tumors are imaged as follows: mice anesthetized by isoflurane inhalation are injected intraperitoneally with D-luciferin (50 mg/kg). Photonic emission is imaged with the in vivo imaging system. Tumor bioluminescence is quantified by integrating the photonic flux (photons per second) through a region encircling each tumor using the Living Image software package. Administration of D-luciferin and detection of tumor bioluminescence in Lck/Pten^fl/fl/Gt(ROSA)26Sor^tm1(Luc)Kael/J mice are performed in a similar manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only.*
References	[1]. Subramaniam Prem S, et al. Targeting nonclassical oncogenes for therapy in T-ALL. Cancer cell (2012), 21(4), 459-72. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1602 mL	10.8008 mL	21.6015 mL	54.0038 mL
	5 mM	0.4320 mL	2.1602 mL	4.3203 mL	10.8008 mL
	10 mM	0.2160 mL	1.0801 mL	2.1602 mL	5.4004 mL
	15 mM	0.1440 mL	0.7201 mL	1.4401 mL	3.6003 mL
	20 mM	0.1080 mL	0.5400 mL	1.0801 mL	2.7002 mL
	25 mM	0.0864 mL	0.4320 mL	0.8641 mL	2.1602 mL
	30 mM	0.0720 mL	0.3600 mL	0.7201 mL	1.8001 mL
	40 mM	0.0540 mL	0.2700 mL	0.5400 mL	1.3501 mL
	50 mM	0.0432 mL	0.2160 mL	0.4320 mL	1.0801 mL
	60 mM	0.0360 mL	0.1800 mL	0.3600 mL	0.9001 mL
	80 mM	0.0270 mL	0.1350 mL	0.2700 mL	0.6750 mL
	100 mM	0.0216 mL	0.1080 mL	0.2160 mL	0.5400 mL