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MedKoo Cat#: 205746 | Name: Taselisib (GDC0032)
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Taselisib, also known as GDC0032 or RG7606, is a selective, potent, orally bioavailable inhibitor of PI3Ka with a Ki = 0.2nM, and with reduced inhibitory activity against PI3Kβ. This selectivity profile, and excellent pharmacokinetic and pharmaceutical properties, allowed for greater efficacy in vivo at the maximum tolerated dose relative to a pan Class I PI3K inhibitor in PIK3CA mutant xenografts. Notably, GDC-0032 preferentially inhibited PIK3CA mutant cells relative to cells with wild-type PI3K. GDC-0032 potently inhibits signal transduction downstream of PI3K and induces apoptosis at low concentrations in breast cancer cell lines and xenograft models that harbor PIK3CA mutations.

Chemical Structure

Taselisib (GDC0032)
Taselisib (GDC0032)
CAS#1282512-48-4

Theoretical Analysis

MedKoo Cat#: 205746

Name: Taselisib (GDC0032)

CAS#: 1282512-48-4

Chemical Formula: C24H28N8O2

Exact Mass: 460.2335

Molecular Weight: 460.53

Elemental Analysis: C, 62.59; H, 6.13; N, 24.33; O, 6.95

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to Ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 4,250.00 Ready to ship
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Synonym
GDC0032, GDC0032, GDC 0032, RG7604, RG7604, RG 7604, Taselisib
IUPAC/Chemical Name
2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide
InChi Key
BEUQXVWXFDOSAQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H28N8O2/c1-14(2)32-22(27-15(3)29-32)19-13-30-8-9-34-20-10-16(6-7-18(20)21(30)28-19)17-11-26-31(12-17)24(4,5)23(25)33/h6-7,10-14H,8-9H2,1-5H3,(H2,25,33)
SMILES Code
CC(C)(N1N=CC(C2=CC=C3C4=NC(C5=NC(C)=NN5C(C)C)=CN4CCOC3=C2)=C1)C(N)=O
Appearance
White to off-white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
In vitro activity:
Phosphorylated HER2 (pHER2), along with phosphorylated HER3 and phosphorylated EGFR, were induced following taselisib treatment in both the HER2+/PIK3CAWT AU565 and the HER2+/PIK3CAmut KPL-4 cells (Fig. 2C). Immunoblot analysis of a larger subset of HER2+ cell lines confirmed a consistent pattern of pHER2 upregulation following taselisib treatment in HER2+/PIK3CAmut cells, but this was not seen in HER2+/PIK3CAWT cells (Fig. 2D). PI3K pathway suppression and induction of apoptosis, as assessed by cleaved PARP and cleaved caspase 3, was induced by inhibition with the dual EGFR and HER2 inhibitor lapatinib in the HER2+/PIK3CAWT cell lines, whereas these effects were primarily induced by PI3K inhibition in the HER2+/PIK3CAmut cell lines (Fig. 2D; Supplementary Fig. S2B). Reference: Mol Cancer Ther. 2020 Jan;19(1):292-303. https://mct.aacrjournals.org/content/19/1/292.long
In vivo activity:
Ten mice were randomized in two groups, control and taselisib. No signs of general toxicity were seen in any of the 2 treatment groups harboring the USC-xenograft and no animal died during the experiments or had to be prematurely sacrificed due to signs of systemic drug toxicity. One mouse in the control group had to be sacrificed after 7 days because it reached 1 cm3 in tumor volume while the remaining control animals had to be sacrificed within 2 weeks secondary to their tumor volume. Taselisib group showed a significant tumor growth inhibition after 14 days of treatment (P=0.007; Figure 5 panel A) and significantly improved OS when compared to the control group (P<0.0001; Figure 5 panel B). The mean survival of the taselisib-treated mice was 45 days. Reference: Gynecol Oncol. 2014 Nov; 135(2): 312–317. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4270135/
Solvent mg/mL mM
Solubility
DMSO 63.3 137.52
Ethanol 7.0 15.20
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 460.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Moore HM, Savage HM, O'Brien C, Zhou W, Sokol ES, Goldberg ME, Metcalfe C, Friedman LS, Lackner MR, Wilson TR. Predictive and Pharmacodynamic Biomarkers of Response to the Phosphatidylinositol 3-Kinase Inhibitor Taselisib in Breast Cancer Preclinical Models. Mol Cancer Ther. 2020 Jan;19(1):292-303. doi: 10.1158/1535-7163.MCT-19-0284. Epub 2019 Sep 18. PMID: 31534012. 2. Lopez S, Schwab CL, Cocco E, Bellone S, Bonazzoli E, English DP, Schwartz PE, Rutherford T, Angioli R, Santin AD. Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo. Gynecol Oncol. 2014 Nov;135(2):312-7. doi: 10.1016/j.ygyno.2014.08.024. Epub 2014 Aug 27. PMID: 25172762; PMCID: PMC4270135. 3. Ndubaku CO, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG. Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610. doi: 10.1021/jm4003632. Epub 2013 Jun 3. PMID: 23662903.
In vitro protocol:
1. Moore HM, Savage HM, O'Brien C, Zhou W, Sokol ES, Goldberg ME, Metcalfe C, Friedman LS, Lackner MR, Wilson TR. Predictive and Pharmacodynamic Biomarkers of Response to the Phosphatidylinositol 3-Kinase Inhibitor Taselisib in Breast Cancer Preclinical Models. Mol Cancer Ther. 2020 Jan;19(1):292-303. doi: 10.1158/1535-7163.MCT-19-0284. Epub 2019 Sep 18. PMID: 31534012. 2. Lopez S, Schwab CL, Cocco E, Bellone S, Bonazzoli E, English DP, Schwartz PE, Rutherford T, Angioli R, Santin AD. Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo. Gynecol Oncol. 2014 Nov;135(2):312-7. doi: 10.1016/j.ygyno.2014.08.024. Epub 2014 Aug 27. PMID: 25172762; PMCID: PMC4270135.
In vivo protocol:
1. Lopez S, Schwab CL, Cocco E, Bellone S, Bonazzoli E, English DP, Schwartz PE, Rutherford T, Angioli R, Santin AD. Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo. Gynecol Oncol. 2014 Nov;135(2):312-7. doi: 10.1016/j.ygyno.2014.08.024. Epub 2014 Aug 27. PMID: 25172762; PMCID: PMC4270135. 2. Ndubaku CO, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG. Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610. doi: 10.1021/jm4003632. Epub 2013 Jun 3. PMID: 23662903.
1: Matus MF, Häkkinen H. Rational Design of Targeted Gold Nanoclusters with High Affinity to Integrin αvβ3 for Combination Cancer Therapy. Bioconjug Chem. 2024 Jul 15. doi: 10.1021/acs.bioconjchem.4c00248. Epub ahead of print. PMID: 39008847. 2: Moein A, Jin JY, Wright MR, Wong H. Quantitative characterization of the effects of fulvestrant alone or in combination with taselisib (PI3Kinase inhibitor) on longitudinal tumor growth in patients with estrogen receptor- positive, HER2-negative, PIK3CA-mutant, advanced or metastatic breast cancer. Cancer Chemother Pharmacol. 2024 Sep;94(3):421-436. doi: 10.1007/s00280-024-04690-4. Epub 2024 Jun 27. PMID: 38937298. 3: Li S, Chao H, Li Z, Chen S, Zhang J, Hao W, Zhang S, Liu C, Liu H. Sex dimorphism of IL-17-secreting peripheral blood mononuclear cells in ankylosing spondylitis based on bioinformatics analysis and machine learning. BMC Musculoskelet Disord. 2024 Jun 24;25(1):490. doi: 10.1186/s12891-024-07589-6. PMID: 38914997; PMCID: PMC11194900. 4: Grinshpun A, Ren S, Graham N, DeMeo MK, Wrabel E, Carter J, Tayob N, Pereslete A, Hamilton E, Juric D, Mayer EL, Tolaney SM, Krop IE, Metzger O. Phase Ib dose-escalation trial of taselisib (GDC-0032) in combination with HER2-directed therapies in patients with advanced HER2+ breast cancer. ESMO Open. 2024 Jun;9(6):103465. doi: 10.1016/j.esmoop.2024.103465. Epub 2024 Jun 3. PMID: 38833970; PMCID: PMC11179085. 5: Yao CY, Lin CC, Wang YH, Kao CJ, Tsai CH, Hou HA, Tien HF, Hsu CL, Chou WC. Kinome expression profiling improves risk stratification and therapeutic targeting in myelodysplastic syndromes. Blood Adv. 2024 May 28;8(10):2442-2454. doi: 10.1182/bloodadvances.2023011512. PMID: 38527292; PMCID: PMC11112608. 6: Pu L, Sun Y, Pu C, Zhang X, Wang D, Liu X, Guo P, Wang B, Xue L, Sun P. Machine learning-based disulfidptosis-related lncRNA signature predicts prognosis, immune infiltration and drug sensitivity in hepatocellular carcinoma. Sci Rep. 2024 Feb 22;14(1):4354. doi: 10.1038/s41598-024-54115-8. PMID: 38388539; PMCID: PMC10883983. 7: Dubey R, Sharma A, Gupta S, Gupta GD, Asati V. A comprehensive review of small molecules targeting PI3K pathway: Exploring the structural development for the treatment of breast cancer. Bioorg Chem. 2024 Feb;143:107077. doi: 10.1016/j.bioorg.2023.107077. Epub 2023 Dec 30. PMID: 38176377. 8: Wang Y, Ji L, Ji C, Wang F. Multi-omics approaches establishing histone modification based prognostic model in glioma patients and further verification of the carcinogenesis mechanism. Funct Integr Genomics. 2023 Sep 21;23(4):307. doi: 10.1007/s10142-023-01229-3. PMID: 37730879. 9: Xie P, Tan SY, Li HF, Tang HD, Zhou JH. Transcriptome data-based status of PI3K/AKT/mTOR pathway indicates heterogeneity and immune modulation in patients with pancreatic ductal adenocarcinoma. J Gene Med. 2024 Jan;26(1):e3570. doi: 10.1002/jgm.3570. Epub 2023 Jul 22. PMID: 37482968. 10: Lian X, Liu B, Wang C, Wang S, Zhuang Y, Li X. Assessing of programmed cell death gene signature for predicting ovarian cancer prognosis and treatment response. Front Endocrinol (Lausanne). 2023 Jun 5;14:1182776. doi: 10.3389/fendo.2023.1182776. PMID: 37342266; PMCID: PMC10277615. 11: You HP, Xu CJ, Zhang LH, Chen ZY, Liu WF, Wang HG, He HF, Zhang LC. Taselisib moderates neuropathic pain through PI3K/AKT signaling pathway in a rat model of chronic constriction injury. Brain Res Bull. 2023 Jul;199:110671. doi: 10.1016/j.brainresbull.2023.110671. Epub 2023 May 18. PMID: 37210013. 12: Hutchinson KE, Chen JW, Savage HM, Stout TJ, Schimmoller F, Cortés J, Dent S, Harbeck N, Jacot W, Krop I, Trabucco SE, Sivakumar S, Sokol ES, Wilson TR. Multiple PIK3CA mutation clonality correlates with outcomes in taselisib + fulvestrant-treated ER+/HER2-, PIK3CA-mutated breast cancers. Genome Med. 2023 Apr 26;15(1):28. doi: 10.1186/s13073-023-01181-8. PMID: 37101291; PMCID: PMC10131374. 13: Fiascarelli A, Merlino G, Capano S, Talucci S, Bisignano D, Bressan A, Bellarosa D, Carrisi C, Paoli A, Bigioni M, Tunici P, Irrissuto C, Salerno M, Arribas J, de Stanchina E, Scaltriti M, Binaschi M. Antitumor activity of the PI3K δ-sparing inhibitor MEN1611 in PIK3CA mutated, trastuzumab-resistant HER2 + breast cancer. Breast Cancer Res Treat. 2023 May;199(1):13-23. doi: 10.1007/s10549-023-06895-2. Epub 2023 Mar 13. PMID: 36913051; PMCID: PMC10147754. 14: Chen JW, Jacot W, Cortés J, Krop IE, Dent S, Harbeck N, De Laurentiis M, Diéras V, Im YH, Stout TJ, Schimmoller F, Savage HM, Hutchinson KE, Wilson TR. ER+, HER2- advanced breast cancer treated with taselisib and fulvestrant: genomic landscape and associated clinical outcomes. Mol Oncol. 2023 Oct;17(10):2000-2016. doi: 10.1002/1878-0261.13416. Epub 2023 Mar 25. PMID: 36892268; PMCID: PMC10552898. 15: Ma S, Cho S, Sahasranaman S, Zhao W, Pang J, Ding X, Dean B, Wang B, Hsu JY, Ware J, Salphati L. Absorption, Metabolism, and Excretion of Taselisib (GDC-0032), a Potent β-Sparing PI3K Inhibitor in Rats, Dogs, and Humans. Drug Metab Dispos. 2023 Apr;51(4):436-450. doi: 10.1124/dmd.122.001096. Epub 2023 Jan 9. PMID: 36623882. 16: Wang S, Li H, Liu J, Zhang Q, Xu W, Xiang J, Fang L, Xu P, Li Z. Integrative analysis of m3C associated genes reveals METTL2A as a potential oncogene in breast Cancer. J Transl Med. 2022 Oct 20;20(1):476. doi: 10.1186/s12967-022-03683-2. PMID: 36266694; PMCID: PMC9583565. 17: Zheng C, Zhang G, Xie K, Diao Y, Luo C, Wang Y, Shen Y, Xue Q. Pan-Cancer Analysis and Experimental Validation Identify ACOT7 as a Novel Oncogene and Potential Therapeutic Target in Lung Adenocarcinoma. Cancers (Basel). 2022 Sep 18;14(18):4522. doi: 10.3390/cancers14184522. PMID: 36139682; PMCID: PMC9497106. 18: Cocco S, Leone A, Roca MS, Lombardi R, Piezzo M, Caputo R, Ciardiello C, Costantini S, Bruzzese F, Sisalli MJ, Budillon A, De Laurentiis M. Inhibition of autophagy by chloroquine prevents resistance to PI3K/AKT inhibitors and potentiates their antitumor effect in combination with paclitaxel in triple negative breast cancer models. J Transl Med. 2022 Jun 27;20(1):290. doi: 10.1186/s12967-022-03462-z. PMID: 35761360; PMCID: PMC9235112. 19: Muranushi H, Shindo T, Chen-Yoshikawa TF, Yoshizawa A, Thi Ngo H, Gochi F, Date H, Takaori-Kondo A. Dual inhibition of the MEK/ERK and PI3K/AKT pathways prevents pulmonary GVHD suppressing perivenulitis and bronchiolitis. Blood Adv. 2023 Jan 10;7(1):106-121. doi: 10.1182/bloodadvances.2021006678. PMID: 35468620; PMCID: PMC9830178. 20: Krop IE, Jegede OA, Grilley-Olson JE, Lauring JD, Mitchell EP, Zwiebel JA, Gray RJ, Wang V, McShane LM, Rubinstein LV, Patton D, Williams PM, Hamilton SR, Kono SA, Ford JM, Garcia AA, Sui XD, Siegel RD, Slomovitz BM, Conley BA, Arteaga CL, Harris LN, O'Dwyer PJ, Chen AP, Flaherty KT. Phase II Study of Taselisib in PIK3CA-Mutated Solid Tumors Other Than Breast and Squamous Lung Cancer: Results From the NCI-MATCH ECOG-ACRIN Trial (EAY131) Subprotocol I. JCO Precis Oncol. 2022 Feb;6:e2100424. doi: 10.1200/PO.21.00424. Erratum in: JCO Precis Oncol. 2022 Mar;6:e2200116. doi: 10.1200/PO.22.00116. PMID: 35138919; PMCID: PMC8865530.