WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H562026
CAS#: 1532533-78-0 (HCl)
Description: TGR-1202 HCl is a potent PI3Kδ inhibitor.
Hodoodo Cat#: H562026
Name: TGR-1202 HCl
CAS#: 1532533-78-0 (HCl)
Chemical Formula: C31H25ClF3N5O3
Exact Mass: 607.16
Molecular Weight: 608.010
Elemental Analysis: C, 61.24; H, 4.14; Cl, 5.83; F, 9.37; N, 11.52; O, 7.89
This product is not in stock, which may be available by custom synthesis.
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Related CAS #: 1532533-67-7 (free base) 1532533-75-7 (sulfate) 1532533-78-0 (HCl)
Synonym: TGR-1202 hydrochloride; TGR 1202 hydrochloride; TGR1202 hydrochloride; TGR-1202 HCl; TGR 1202 HCl; TGR1202 HCl;
IUPAC/Chemical Name: 2-[(1S)-1-[4-Amino-3-(3-fluoro-4-propan-2-yloxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)chromen-4-one hydrochloride
InChi Key: QGVUVMVWYWMZIR-NTISSMGPSA-N
InChi Code: InChI=1S/C31H24F3N5O3.ClH/c1-15(2)41-24-9-7-18(12-22(24)34)27-26-30(35)36-14-37-31(26)39(38-27)16(3)29-25(17-5-4-6-19(32)11-17)28(40)21-13-20(33)8-10-23(21)42-29;/h4-16H,1-3H3,(H2,35,36,37);1H/t16-;/m0./s1
SMILES Code: O=C1C(C2=CC=CC(F)=C2)=C([C@@H](N3N=C(C4=CC=C(OC(C)C)C(F)=C4)C5=C(N)N=CN=C53)C)OC6=C1C=C(F)C=C6.[H]Cl
Appearance: 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
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: | |
| In vitro activity: | |
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The following data is based on the product molecular weight 608.01 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.
| 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: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Robak P, Robak T. Novel synthetic drugs currently in clinical development for chronic lymphocytic leukemia. Expert Opin Investig Drugs. 2017 Nov;26(11):1249-1265. doi: 10.1080/13543784.2017.1384814. Epub 2017 Oct 3. Review. PubMed PMID: 28942659.
2: Zinzani PL, Broccoli A. Possible novel agents in marginal zone lymphoma. Best Pract Res Clin Haematol. 2017 Mar - Jun;30(1-2):149-157. doi: 10.1016/j.beha.2016.07.003. Epub 2016 Nov 4. Review. PubMed PMID: 28288710.
3: Deng C, Lipstein MR, Scotto L, Jirau Serrano XO, Mangone MA, Li S, Vendome J, Hao Y, Xu X, Deng SX, Realubit RB, Tatonetti NP, Karan C, Lentzsch S, Fruman DA, Honig B, Landry DW, O'Connor OA. Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies. Blood. 2017 Jan 5;129(1):88-99. doi: 10.1182/blood-2016-08-731240. Epub 2016 Oct 26. PubMed PMID: 27784673; PubMed Central PMCID: PMC5216267.
4: Locatelli SL, Careddu G, Inghirami G, Castagna L, Sportelli P, Santoro A, Carlo-Stella C. The novel PI3K-δ inhibitor TGR-1202 enhances Brentuximab Vedotin-induced Hodgkin lymphoma cell death via mitotic arrest. Leukemia. 2016 Dec;30(12):2402-2405. doi: 10.1038/leu.2016.224. Epub 2016 Aug 8. PubMed PMID: 27499137.
5: Brown JR. The PI3K pathway: clinical inhibition in chronic lymphocytic leukemia. Semin Oncol. 2016 Apr;43(2):260-4. doi: 10.1053/j.seminoncol.2016.02.004. Epub 2016 Feb 8. Review. PubMed PMID: 27040704.
