SRX3207
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MedKoo CAT#: 408146

CAS#: 2254693-15-5

Description: SRX3207 is a Novel Dual Syk-PI3K Inhibitory Chemotype Relieves Tumor Immunosuppression with IC50 of 39.9 nM. SRX3207 demonstrates efficacy in multiple tumor models and represents a novel combinatorial approach to activate antitumor immunity. SRX3207 potently inhibited Syk and PI3K signaling and augmented the anti-tumor immune response in lung carcinoma tumor model with no toxicity.


Chemical Structure

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SRX3207
CAS# 2254693-15-5

Theoretical Analysis

MedKoo Cat#: 408146
Name: SRX3207
CAS#: 2254693-15-5
Chemical Formula: C29H29N7O3S
Exact Mass: 555.21
Molecular Weight: 555.660
Elemental Analysis: C, 62.69; H, 5.26; N, 17.65; O, 8.64; S, 5.77

Price and Availability

Size Price Availability Quantity
25mg USD 550 2 Weeks
50mg USD 950 2 Weeks
100mg USD 1650 2 Weeks
200mg USD 2650 2 Weeks
500mg USD 3950 2 Weeks
1g USD 4950 2 Weeks
2g USD 7950 2 Weeks
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Related CAS #: 2254693-15-5    

Synonym: SRX3207; SRX-3207; SRX 3207;

IUPAC/Chemical Name: 3-[4-[[4-[4-(1-Azetidinylmethyl)-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]phenyl]-5-(4-morpholinyl)-7H-thieno[3,2-b]pyran-7-one

InChi Key: ZZVOPDBZUNUMPR-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H29N7O3S/c1-19-21(16-34-9-2-10-34)17-36(33-19)25-7-8-30-29(32-25)31-22-5-3-20(4-6-22)23-18-40-28-24(37)15-26(39-27(23)28)35-11-13-38-14-12-35/h3-8,15,17-18H,2,9-14,16H2,1H3,(H,30,31,32)

SMILES Code: O=C1C2=C(C(C3=CC=C(NC4=NC=CC(N5N=C(C)C(CN6CCC6)=C5)=N4)C=C3)=CS2)OC(N7CCOCC7)=C1

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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: Macrophages (MΦ) play a critical role in tumor growth, immunosuppression, and inhibition of adaptive immune responses in cancer. Hence, targeting signaling pathways in MΦs that promote tumor immunosuppression will provide therapeutic benefit. PI3Kγ has been recently established by our group and others as a novel immuno-oncology target.

Product Data:
Biological target: SRX3207 is a Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively.
In vitro activity: This study developed in silico the dual Syk/PI3K inhibitor, SRX3207, for the combinatorial inhibition of Syk and PI3K in one small molecule. Reference: Mol Cancer Ther. 2020 Mar;19(3):755-764. https://pubmed.ncbi.nlm.nih.gov/31974273/
In vivo activity: To be determined

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5.0 9.00

Preparing Stock Solutions

The following data is based on the product molecular weight 555.66 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. Joshi S, Liu KX, Zulcic M, Singh AR, Skola D, Glass CK, Sanders PD, Sharabi AB, Pham TV, Tamayo P, Shiang D, Dinh HQ, Hedrick CC, Morales GA, Garlich JR, Durden DL. Macrophage Syk-PI3Kγ Inhibits Antitumor Immunity: SRX3207, a Novel Dual Syk-PI3K Inhibitory Chemotype Relieves Tumor Immunosuppression. Mol Cancer Ther. 2020 Mar;19(3):755-764. doi: 10.1158/1535-7163.MCT-19-0947. Epub 2020 Jan 23. PMID: 31974273; PMCID: PMC7450492.
In vitro protocol: 1. Joshi S, Liu KX, Zulcic M, Singh AR, Skola D, Glass CK, Sanders PD, Sharabi AB, Pham TV, Tamayo P, Shiang D, Dinh HQ, Hedrick CC, Morales GA, Garlich JR, Durden DL. Macrophage Syk-PI3Kγ Inhibits Antitumor Immunity: SRX3207, a Novel Dual Syk-PI3K Inhibitory Chemotype Relieves Tumor Immunosuppression. Mol Cancer Ther. 2020 Mar;19(3):755-764. doi: 10.1158/1535-7163.MCT-19-0947. Epub 2020 Jan 23. PMID: 31974273; PMCID: PMC7450492.
In vivo protocol: To be determined

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Joshi S, Liu KX, Zulcic M, Singh AR, Skola D, Glass CK, Sanders PD, Sharabi AB, Pham TV, Tamayo P, Shiang D, Dinh HQ, Hedrick CC, Morales GA, Garlich JR, Durden DL. Macrophage Syk-PI3Kγ Inhibits Antitumor Immunity: SRX3207, a Novel Dual Syk-PI3K Inhibitory Chemotype Relieves Tumor Immunosuppression. Mol Cancer Ther. 2020 Mar;19(3):755-764. doi: 10.1158/1535-7163.MCT-19-0947. Epub 2020 Jan 23. PMID: 31974273; PMCID: PMC7450492.